Ligand source activities (1 row/activity)





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DOI

54582892 68374 0 None 3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 514 12 1 5 6.0 O=C(NC1CC1)c1ccc(OCCCC2CC2CCCC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771104 68374 0 None 3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 514 12 1 5 6.0 O=C(NC1CC1)c1ccc(OCCCC2CC2CCCC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
89584034 165485 0 None 3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 10 0 6 4.0 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3cc(F)c(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
CHEMBL4093284 165485 0 None 3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 10 0 6 4.0 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3cc(F)c(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
89584002 166495 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4104464 166495 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCC1 10.1016/j.bmcl.2017.01.091
54587813 68369 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771098 68369 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
117678530 165924 0 None 2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 466 9 0 5 4.3 CCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
CHEMBL4098051 165924 0 None 2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 466 9 0 5 4.3 CCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
89584002 166495 0 None -1 2 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4104464 166495 0 None -1 2 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCC1 10.1016/j.bmcl.2017.01.091
54587813 68369 0 None 1 2 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771098 68369 0 None 1 2 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
145949889 169597 0 None 229 2 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 536 7 1 10 3.1 COc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1C[C@@H]2COC[C@@H](C1)N2C(=O)OC1(C)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4172551 169597 0 None 229 2 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 536 7 1 10 3.1 COc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1C[C@@H]2COC[C@@H](C1)N2C(=O)OC1(C)CC1 10.1021/acsmedchemlett.8b00073
53630410 7928 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5739 7928 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1773283 7928 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
118720405 122662 0 None 15 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 465 5 0 5 5.4 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354778 122662 0 None 15 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 465 5 0 5 5.4 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
71573174 162692 0 None 1 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 8 0 5 4.2 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4060838 162692 0 None 1 2 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 8 0 5 4.2 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)N1CCC1 10.1016/j.bmcl.2017.01.091
54582152 7827 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 507 4 1 9 2.4 O=C(N1CCC(CC1)Oc1ncnc2c1[nH]c(=O)n2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5740 7827 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 507 4 1 9 2.4 O=C(N1CCC(CC1)Oc1ncnc2c1[nH]c(=O)n2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1773292 7827 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 507 4 1 9 2.4 O=C(N1CCC(CC1)Oc1ncnc2c1[nH]c(=O)n2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
134136399 149667 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 523 7 1 10 3.6 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3893596 149667 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 523 7 1 10 3.6 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
24939268 7240 67 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2011.03.007
5653 7240 67 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2011.03.007
CHEMBL461384 7240 67 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2011.03.007
24939268 7240 67 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1021/jm8006867
5653 7240 67 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1021/jm8006867
CHEMBL461384 7240 67 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1021/jm8006867
11397354 7839 2 None 23 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5741 7839 2 None 23 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1773293 7839 2 None 23 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
89584118 164077 0 None 2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 482 10 0 6 3.9 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
CHEMBL4077033 164077 0 None 2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 482 10 0 6 3.9 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
122191633 130525 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 465 9 0 7 4.2 CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3nc(C(C)C)no3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
CHEMBL3622182 130525 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 465 9 0 7 4.2 CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3nc(C(C)C)no3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
71573174 162692 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 8 0 5 4.2 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4060838 162692 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 8 0 5 4.2 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)N1CCC1 10.1016/j.bmcl.2017.01.091
89584012 164322 0 None 8 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 488 8 1 6 3.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CC(O)C1 10.1016/j.bmcl.2017.01.091
CHEMBL4080222 164322 0 None 8 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 488 8 1 6 3.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CC(O)C1 10.1016/j.bmcl.2017.01.091
89584034 165485 0 None -3 2 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 10 0 6 4.0 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3cc(F)c(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
CHEMBL4093284 165485 0 None -3 2 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 10 0 6 4.0 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3cc(F)c(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
54582892 68374 0 None -3 2 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 514 12 1 5 6.0 O=C(NC1CC1)c1ccc(OCCCC2CC2CCCC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771104 68374 0 None -3 2 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 514 12 1 5 6.0 O=C(NC1CC1)c1ccc(OCCCC2CC2CCCC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
117678530 165924 0 None -2 2 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 466 9 0 5 4.3 CCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
CHEMBL4098051 165924 0 None -2 2 Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 466 9 0 5 4.3 CCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
53630394 7873 0 None 21 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5738 7873 0 None 21 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1775178 7873 0 None 21 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
24961800 68353 0 None 1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
CHEMBL1771081 68353 0 None 1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
49855246 122659 0 None 10 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(C)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
CHEMBL3354774 122659 0 None 10 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(C)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
66964555 117540 0 None 38 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 496 8 0 5 5.0 COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260536 117540 0 None 38 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 496 8 0 5 5.0 COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
11282871 7870 0 None 8 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5737 7870 0 None 8 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1775169 7870 0 None 8 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
71116044 130522 0 None 3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 453 9 0 9 2.8 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622179 130522 0 None 3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 453 9 0 9 2.8 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
53492331 129075 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 549 6 0 8 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C(F)(F)F)C(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598101 129075 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 549 6 0 8 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C(F)(F)F)C(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
137659500 165992 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 537 6 1 10 3.8 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@@H]1C[C@@H]2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4098760 165992 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 537 6 1 10 3.8 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@@H]1C[C@@H]2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
134131905 151917 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 483 5 2 9 4.5 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(C#N)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3912040 151917 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 483 5 2 9 4.5 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(C#N)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
134156958 160604 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 509 7 1 10 3.2 CCOC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3982536 160604 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 509 7 1 10 3.2 CCOC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
71562846 110052 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 537 6 1 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084479 110052 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 537 6 1 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
90148901 130513 0 None 3 2 Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 449 8 0 7 3.1 COc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622170 130513 0 None 3 2 Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 449 8 0 7 3.1 COc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
25053113 197913 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 501 6 1 11 3.6 CC(C)(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL518819 197913 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 501 6 1 11 3.6 CC(C)(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
71135255 130508 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 430 8 0 7 2.9 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622166 130508 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 430 8 0 7 2.9 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
89584050 163573 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 8 0 5 5.1 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCCCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4070965 163573 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 8 0 5 5.1 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCCCC1 10.1016/j.bmcl.2017.01.091
134142930 152229 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 536 6 2 10 4.0 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3914281 152229 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 536 6 2 10 4.0 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
134147992 156882 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 537 6 1 10 4.0 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3951013 156882 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 537 6 1 10 4.0 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
71562846 110052 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 537 6 1 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084479 110052 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 537 6 1 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
71562724 110055 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 536 6 2 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084483 110055 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 536 6 2 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
89583782 164622 0 None 1 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 9 1 5 4.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)NC1CC1 10.1016/j.bmcl.2017.01.091
CHEMBL4083676 164622 0 None 1 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 9 1 5 4.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)NC1CC1 10.1016/j.bmcl.2017.01.091
134135618 150942 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 515 7 1 10 2.0 CS(=O)(=O)c1ccc(Nc2ncnc(OC3C[C@H]4CC[C@H](C3)N4S(C)(=O)=O)c2[N+](=O)[O-])c(F)c1 10.1016/j.bmc.2016.10.030
CHEMBL3904015 150942 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 515 7 1 10 2.0 CS(=O)(=O)c1ccc(Nc2ncnc(OC3C[C@H]4CC[C@H](C3)N4S(C)(=O)=O)c2[N+](=O)[O-])c(F)c1 10.1016/j.bmc.2016.10.030
89584118 164077 0 None -2 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 482 10 0 6 3.9 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
CHEMBL4077033 164077 0 None -2 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 482 10 0 6 3.9 COCc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)nc1 10.1016/j.bmcl.2017.01.091
117684497 166037 0 None 1 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4099186 166037 0 None 1 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1)N1CCC1 10.1016/j.bmcl.2017.01.091
71136686 130510 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 441 8 0 9 3.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
CHEMBL3622168 130510 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 441 8 0 9 3.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
71128813 130514 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 463 9 0 7 3.5 CCOc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622171 130514 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 463 9 0 7 3.5 CCOc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
122191632 130524 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 465 9 0 7 4.4 CCS(=O)(=O)c1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3nc(C(C)C)no3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
CHEMBL3622181 130524 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 465 9 0 7 4.4 CCS(=O)(=O)c1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3nc(C(C)C)no3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
156012977 184294 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells preincubated for 30 mins followed by d2 cAMP addition and measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells preincubated for 30 mins followed by d2 cAMP addition and measured after 60 mins by HTRF assay
ChEMBL 412 4 0 7 4.7 Cc1cc(-c2ccc(N3CCC(c4nc(C(C)C)no4)CC3)nc2)c(C#N)cc1C#N 10.1021/acs.jmedchem.9b01840
CHEMBL4639701 184294 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells preincubated for 30 mins followed by d2 cAMP addition and measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells preincubated for 30 mins followed by d2 cAMP addition and measured after 60 mins by HTRF assay
ChEMBL 412 4 0 7 4.7 Cc1cc(-c2ccc(N3CCC(c4nc(C(C)C)no4)CC3)nc2)c(C#N)cc1C#N 10.1021/acs.jmedchem.9b01840
71474021 130507 0 None 1 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 483 9 1 7 3.1 O=S(=O)(CCO)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
CHEMBL3622165 130507 0 None 1 2 Mouse 8.8 pEC50 = 8.8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 483 9 1 7 3.1 O=S(=O)(CCO)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
137649810 164167 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 536 6 2 10 3.9 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4078300 164167 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 536 6 2 10 3.9 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
89583782 164622 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 9 1 5 4.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)NC1CC1 10.1016/j.bmcl.2017.01.091
CHEMBL4083676 164622 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 454 9 1 5 4.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1)NC1CC1 10.1016/j.bmcl.2017.01.091
71116039 130518 0 None 1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622175 130518 0 None 1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
145968038 171719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 432 5 0 10 2.1 N#Cc1cnccc1COc1cnc(N2CCN(c3noc(C(F)(F)F)n3)CC2)nc1 10.1016/j.bmc.2018.04.004
CHEMBL4224878 171719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 432 5 0 10 2.1 N#Cc1cnccc1COc1cnc(N2CCN(c3noc(C(F)(F)F)n3)CC2)nc1 10.1016/j.bmc.2018.04.004
86694581 141136 0 None - 1 Human 8.0 pEC50 = 8 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 459 4 0 6 3.7 CC1(OC(=O)N2CCC(c3cc4cc(C5=CCN(S(C)(=O)=O)CC5)ncc4o3)CC2)CC1 nan
CHEMBL3717304 141136 0 None - 1 Human 8.0 pEC50 = 8 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 459 4 0 6 3.7 CC1(OC(=O)N2CCC(c3cc4cc(C5=CCN(S(C)(=O)=O)CC5)ncc4o3)CC2)CC1 nan
25053042 179764 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 473 7 1 11 2.9 CCc1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL451793 179764 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 473 7 1 11 2.9 CCc1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
127050518 147762 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 510 5 0 7 4.5 CC(C)(OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc32)CC1)C(F)F 10.1016/j.bmcl.2016.06.050
CHEMBL3823396 147762 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 510 5 0 7 4.5 CC(C)(OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc32)CC1)C(F)F 10.1016/j.bmcl.2016.06.050
127048492 147815 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 471 5 1 6 4.3 CCNC(=O)c1cc(F)c(-c2cc3cnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmcl.2016.06.050
CHEMBL3824019 147815 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 471 5 1 6 4.3 CCNC(=O)c1cc(F)c(-c2cc3cnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmcl.2016.06.050
127048492 147815 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 471 5 1 6 4.3 CCNC(=O)c1cc(F)c(-c2cc3cnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
CHEMBL3824019 147815 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 471 5 1 6 4.3 CCNC(=O)c1cc(F)c(-c2cc3cnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
137633747 163133 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 492 6 1 8 3.7 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(F)c1F 10.1016/j.bmc.2017.06.014
CHEMBL4065926 163133 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 492 6 1 8 3.7 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(F)c1F 10.1016/j.bmc.2017.06.014
145957126 168803 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 487 5 1 8 3.9 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4159767 168803 0 None 5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 487 5 1 8 3.9 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
68036931 168999 0 None 6 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 487 5 1 8 3.9 N#Cc1ccc(Nc2ncnc(OC3C4COCC3CN(C(=O)OC3CCC3)C4)c2F)c(Cl)c1 10.1021/acsmedchemlett.8b00073
CHEMBL4163003 168999 0 None 6 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 487 5 1 8 3.9 N#Cc1ccc(Nc2ncnc(OC3C4COCC3CN(C(=O)OC3CCC3)C4)c2F)c(Cl)c1 10.1021/acsmedchemlett.8b00073
68036809 169675 0 None 6 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 501 5 1 8 4.3 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CCC1 10.1021/acsmedchemlett.8b00073
CHEMBL4173709 169675 0 None 6 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 501 5 1 8 4.3 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CCC1 10.1021/acsmedchemlett.8b00073
145972319 171362 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 404 9 0 4 4.6 CC(C)OC(=O)N1CCC(CCCCCOc2ccc(C(=O)N(C)C)cc2)CC1 10.1016/j.bmcl.2018.02.044
CHEMBL4215560 171362 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 404 9 0 4 4.6 CC(C)OC(=O)N1CCC(CCCCCOc2ccc(C(=O)N(C)C)cc2)CC1 10.1016/j.bmcl.2018.02.044
118722572 122932 0 None 7 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 470 5 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2C#N)cn1 10.1021/jm5011012
CHEMBL3357996 122932 0 None 7 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 470 5 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2C#N)cn1 10.1021/jm5011012
66964295 117538 0 None 7 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260533 117538 0 None 7 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
24896778 89295 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 494 5 0 8 3.8 CC(C)SC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177762 89295 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 494 5 0 8 3.8 CC(C)SC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
51030898 84235 0 None 9 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1noc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)n1 10.1021/jm300310c
CHEMBL2087084 84235 0 None 9 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1noc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)n1 10.1021/jm300310c
25012362 68365 0 None -1 2 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771094 68365 0 None -1 2 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
89995522 150883 0 None - 1 Human 8.0 pEC50 = 8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 465 5 0 5 4.9 CC(C)(OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1)C(F)(F)F nan
CHEMBL3903582 150883 0 None - 1 Human 8.0 pEC50 = 8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 465 5 0 5 4.9 CC(C)(OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1)C(F)(F)F nan
156017361 184446 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 480 7 0 10 4.0 CCc1cnc(N2CC=C(c3nc(COc4ccc(-n5cnnn5)cc4Cl)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
CHEMBL4641634 184446 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 480 7 0 10 4.0 CCc1cnc(N2CC=C(c3nc(COc4ccc(-n5cnnn5)cc4Cl)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
67950429 90448 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 456 7 0 11 2.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)nc1 10.1021/ml300296q
CHEMBL2204984 90448 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 456 7 0 11 2.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)nc1 10.1021/ml300296q
122184149 129088 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
CHEMBL3598114 129088 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
53492331 129075 0 None -1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 549 6 0 8 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C(F)(F)F)C(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598101 129075 0 None -1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 549 6 0 8 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C(F)(F)F)C(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
57415237 120327 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 489 4 0 8 4.5 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321828 120327 1 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 489 4 0 8 4.5 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
145966434 171039 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 493 7 1 7 4.5 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CCNC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4211588 171039 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 493 7 1 7 4.5 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CCNC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
76335814 111696 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 541 6 0 6 6.9 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4cc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112988 111696 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 541 6 0 6 6.9 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4cc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76310376 111703 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 594 6 0 8 7.1 O=S(=O)(c1ccc(Cl)cc1)N1CCSc2cc(Cl)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112995 111703 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 594 6 0 8 7.1 O=S(=O)(c1ccc(Cl)cc1)N1CCSc2cc(Cl)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76314043 111706 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 492 5 0 6 5.1 COC(=O)c1cc(Cl)nc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)c1 10.1016/j.bmcl.2013.12.127
CHEMBL3112998 111706 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 492 5 0 6 5.1 COC(=O)c1cc(Cl)nc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)c1 10.1016/j.bmcl.2013.12.127
76332170 111707 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 506 6 0 6 5.5 CCOC(=O)c1cc(Cl)nc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)c1 10.1016/j.bmcl.2013.12.127
CHEMBL3112999 111707 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 506 6 0 6 5.5 CCOC(=O)c1cc(Cl)nc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)c1 10.1016/j.bmcl.2013.12.127
76314049 111727 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 526 6 0 7 5.7 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(F)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113019 111727 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 526 6 0 7 5.7 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(F)n3)cc21 10.1016/j.bmcl.2013.12.127
71546855 93018 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 476 5 0 10 3.3 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312515 93018 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 476 5 0 10 3.3 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
58017025 89305 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 5 0 8 3.4 Cc1nc(OC2CCN(C(=O)OC(C)C)CC2)c2c(n1)N(c1ccc(S(C)(=O)=O)cc1F)CC2 10.1021/jm301404a
CHEMBL2177773 89305 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 5 0 8 3.4 Cc1nc(OC2CCN(C(=O)OC(C)C)CC2)c2c(n1)N(c1ccc(S(C)(=O)=O)cc1F)CC2 10.1021/jm301404a
71462835 89835 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 474 5 0 8 3.3 Cc1cc(S(C)(=O)=O)ccc1N1CCc2c(OC3CCN(C(=O)OC(C)C)CC3)ncnc21 10.1021/jm301404a
CHEMBL2181691 89835 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 474 5 0 8 3.3 Cc1cc(S(C)(=O)=O)ccc1N1CCc2c(OC3CCN(C(=O)OC(C)C)CC3)ncnc21 10.1021/jm301404a
46884858 14483 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 482 9 0 7 3.0 CCCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1088852 14483 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 482 9 0 7 3.0 CCCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
60155461 84198 0 None 6 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 8 2.2 C[C@@H]1CN(C(=O)OCC(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086688 84198 0 None 6 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 8 2.2 C[C@@H]1CN(C(=O)OCC(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
90666908 116229 0 None 6 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 464 6 0 12 1.5 C[C@@H]1CN(c2noc(C3COCCO3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220233 116229 0 None 6 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 464 6 0 12 1.5 C[C@@H]1CN(c2noc(C3COCCO3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
122194337 130771 0 None -3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
CHEMBL3629478 130771 0 None -3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
58190329 116195 0 None -1 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 448 6 0 11 1.7 C[C@@H]1CN(c2noc(C3(C)COC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220032 116195 0 None -1 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 448 6 0 11 1.7 C[C@@H]1CN(c2noc(C3(C)COC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
67461265 151822 0 None - 1 Human 7.0 pEC50 = 7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 325 2 1 5 3.7 Cc1ccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)s1 nan
CHEMBL3911265 151822 0 None - 1 Human 7.0 pEC50 = 7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 325 2 1 5 3.7 Cc1ccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)s1 nan
3710394 193342 1 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 472 9 0 11 2.7 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(C(=O)CC(=O)OC)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL487817 193342 1 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 472 9 0 11 2.7 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(C(=O)CC(=O)OC)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
145983613 172631 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 465 4 1 9 4.0 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c(Nc4ccc(C#N)cc4F)ncnc23)CC1 10.1016/j.bmc.2018.06.035
CHEMBL4248913 172631 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 465 4 1 9 4.0 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c(Nc4ccc(C#N)cc4F)ncnc23)CC1 10.1016/j.bmc.2018.06.035
71718289 94502 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 615 8 2 10 5.5 COc1cc2nc(NCC3CC4CCC(C3)N4C(=O)OC(C)(C)C)nc(Nc3ccc(S(C)(=O)=O)cc3F)c2cc1OC 10.1016/j.bmc.2012.12.013
CHEMBL2336753 94502 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 615 8 2 10 5.5 COc1cc2nc(NCC3CC4CCC(C3)N4C(=O)OC(C)(C)C)nc(Nc3ccc(S(C)(=O)=O)cc3F)c2cc1OC 10.1016/j.bmc.2012.12.013
71720096 94503 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 601 6 1 10 4.9 COc1cc2nc(N3CCC4CCC(C3)N4C(=O)OC(C)(C)C)nc(Nc3ccc(S(C)(=O)=O)cc3F)c2cc1OC 10.1016/j.bmc.2012.12.013
CHEMBL2336759 94503 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 601 6 1 10 4.9 COc1cc2nc(N3CCC4CCC(C3)N4C(=O)OC(C)(C)C)nc(Nc3ccc(S(C)(=O)=O)cc3F)c2cc1OC 10.1016/j.bmc.2012.12.013
71717059 94504 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 601 7 2 10 5.3 COc1cc2nc(NC3CC4CCC(C3)N4C(=O)OC(C)(C)C)nc(Nc3ccc(S(C)(=O)=O)cc3F)c2cc1OC 10.1016/j.bmc.2012.12.013
CHEMBL2336769 94504 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 601 7 2 10 5.3 COc1cc2nc(NC3CC4CCC(C3)N4C(=O)OC(C)(C)C)nc(Nc3ccc(S(C)(=O)=O)cc3F)c2cc1OC 10.1016/j.bmc.2012.12.013
57394106 77609 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 449 6 1 9 2.7 Cc1c(Nc2ccc(S(C)(=O)=O)nc2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951023 77609 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 449 6 1 9 2.7 Cc1c(Nc2ccc(S(C)(=O)=O)nc2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
58017047 89312 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 476 5 0 6 4.3 CC(C)OC(=O)N1CCC(Oc2cccc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177780 89312 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 476 5 0 6 4.3 CC(C)OC(=O)N1CCC(Oc2cccc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
46884936 14753 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 509 7 0 7 2.6 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)N4CCCCC4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1090559 14753 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 509 7 0 7 2.6 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)N4CCCCC4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
46884937 14810 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 467 8 1 6 2.2 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)NC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1090879 14810 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 467 8 1 6 2.2 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)NC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
90666912 116234 0 None -5 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 438 6 0 9 2.1 CCC1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
CHEMBL3220239 116234 0 None -5 2 Mouse 6.0 pEC50 = 6 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 438 6 0 9 2.1 CCC1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
57401106 77611 0 None -3 2 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1cc(S(C)(=O)=O)ncc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951025 77611 0 None -3 2 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1cc(S(C)(=O)=O)ncc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
73387823 153602 0 None - 1 Human 6.0 pEC50 = 6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 6 3.5 Cn1ncnc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3924857 153602 0 None - 1 Human 6.0 pEC50 = 6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 6 3.5 Cn1ncnc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
54589191 117655 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 496 8 0 5 3.3 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(S(=O)(=O)CCC)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261124 117655 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 496 8 0 5 3.3 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(S(=O)(=O)CCC)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
140253894 173984 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 602 6 0 6 6.5 CC(C)(OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1016/j.bmcl.2018.08.010
CHEMBL4291700 173984 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 602 6 0 6 6.5 CC(C)(OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1016/j.bmcl.2018.08.010
54589270 117672 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 590 9 1 7 4.5 CCCc1cnc(N2CCC(C3Cc4c(F)c(C5=CCN(S(=O)(=O)CCC(C)(C)O)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261141 117672 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 590 9 1 7 4.5 CCCc1cnc(N2CCC(C3Cc4c(F)c(C5=CCN(S(=O)(=O)CCC(C)(C)O)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
118720411 122667 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 507 5 0 5 6.6 CCOC(=O)C1(Cc2ccccc2)CCCCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354783 122667 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 507 5 0 5 6.6 CCOC(=O)C1(Cc2ccccc2)CCCCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
122184145 129084 0 None -2 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 505 7 0 7 4.2 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598110 129084 0 None -2 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 505 7 0 7 4.2 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
89995529 151650 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 510 6 0 7 4.7 CCOC(=O)c1c(C)nn(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)c1C nan
CHEMBL3909892 151650 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 510 6 0 7 4.7 CCOC(=O)c1c(C)nn(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)c1C nan
62706854 83082 0 None -1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1nnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)o1 10.1016/j.bmcl.2012.05.117
CHEMBL2058671 83082 0 None -1 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1nnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)o1 10.1016/j.bmcl.2012.05.117
89995563 157877 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 395 6 0 5 3.7 C=CCOC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3959129 157877 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 395 6 0 5 3.7 C=CCOC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
89995710 158403 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 433 5 0 6 3.0 CC(C)OC(=O)N1CC[C@@H](N(C(=O)c2ccc(-n3cncn3)c(F)c2)C2CC2)[C@@H](F)C1 nan
CHEMBL3963699 158403 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 433 5 0 6 3.0 CC(C)OC(=O)N1CC[C@@H](N(C(=O)c2ccc(-n3cncn3)c(F)c2)C2CC2)[C@@H](F)C1 nan
71546201 93013 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 451 5 0 8 3.9 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312510 93013 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 451 5 0 8 3.9 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
62706517 83014 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 408 5 1 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)S(=O)(=O)CC3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058402 83014 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 408 5 1 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)S(=O)(=O)CC3)CC1 10.1016/j.bmcl.2012.05.117
54581959 68350 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cnccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771078 68350 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cnccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
25024141 170568 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 442 5 0 9 3.8 CC(C)(C)OC(=O)N1CCC(c2nc(COc3ccc(-n4cnnn4)cc3)cs2)CC1 10.1016/j.bmcl.2017.10.046
CHEMBL4205949 170568 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 442 5 0 9 3.8 CC(C)(C)OC(=O)N1CCC(c2nc(COc3ccc(-n4cnnn4)cc3)cs2)CC1 10.1016/j.bmcl.2017.10.046
71287404 117654 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 476 6 0 5 4.1 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(C(=O)OC(C)C)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261123 117654 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 476 6 0 5 4.1 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(C(=O)OC(C)C)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
51030811 84188 1 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 385 4 0 7 2.8 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
CHEMBL2086677 84188 1 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 385 4 0 7 2.8 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
118711795 120821 0 None -7 2 Rat 7.0 pEC50 = 7.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)(C)F)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326686 120821 0 None -7 2 Rat 7.0 pEC50 = 7.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)(C)F)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
66554759 93760 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 399 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccncc3C#N)CC2)CC1 10.1021/ml300399u
CHEMBL2323600 93760 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 399 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccncc3C#N)CC2)CC1 10.1021/ml300399u
54591265 158962 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 3.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCC4=O)cc3)oc2c1 nan
CHEMBL3968362 158962 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 3.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCC4=O)cc3)oc2c1 nan
67464812 159879 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 10 1 6 5.9 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN(C(C)C)C(C)C)cc4)oc3c2)[C@H]1C nan
CHEMBL3976258 159879 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 10 1 6 5.9 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN(C(C)C)C(C)C)cc4)oc3c2)[C@H]1C nan
76309730 110001 0 None -165 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 452 5 0 7 4.4 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084367 110001 0 None -165 2 Mouse 5.0 pEC50 = 5.0 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 452 5 0 7 4.4 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
118300914 155921 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 486 5 0 5 5.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cnc(-c4ccccc4)c3)cc2)C2CC2)CC1 nan
CHEMBL3943419 155921 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 486 5 0 5 5.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cnc(-c4ccccc4)c3)cc2)C2CC2)CC1 nan
67467232 166629 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CN4CCCCC4)cc3)oc2c1 nan
CHEMBL4106619 166629 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CN4CCCCC4)cc3)oc2c1 nan
71547153 92962 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 497 5 0 7 4.1 Cc1c(Oc2ccc(C(=O)N(C)C)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312160 92962 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 497 5 0 7 4.1 Cc1c(Oc2ccc(C(=O)N(C)C)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71736573 141309 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 470 4 0 6 5.2 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(CS(C)(=O)=O)cc4)ncc3o2)CC1 nan
CHEMBL3717883 141309 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 470 4 0 6 5.2 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(CS(C)(=O)=O)cc4)ncc3o2)CC1 nan
137648824 164488 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 522 7 0 9 4.5 CCc1cnc(N2CCC(Oc3ncnc4c(-c5ccc(C(=O)N(C)OC)c(F)c5)csc34)CC2)nc1 10.1016/j.bmcl.2017.06.032
CHEMBL4081913 164488 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 522 7 0 9 4.5 CCc1cnc(N2CCC(Oc3ncnc4c(-c5ccc(C(=O)N(C)OC)c(F)c5)csc34)CC2)nc1 10.1016/j.bmcl.2017.06.032
118249777 186494 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 546 7 1 9 5.1 Cc1c(Oc2cccc(/C=C3\SC(=O)NC3=O)c2)ncnc1OC1CCN(C(=O)OCc2ccccc2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4743968 186494 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 546 7 1 9 5.1 Cc1c(Oc2cccc(/C=C3\SC(=O)NC3=O)c2)ncnc1OC1CCN(C(=O)OCc2ccccc2)CC1 10.1016/j.bmc.2021.116071
118711785 120812 0 None -15 2 Rat 6.0 pEC50 = 6.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=S)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326677 120812 0 None -15 2 Rat 6.0 pEC50 = 6.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=S)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
51030529 84196 0 None -19 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 421 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C#N)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086686 84196 0 None -19 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 421 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C#N)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
118722582 122944 0 None -13 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
CHEMBL3358007 122944 0 None -13 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
67461046 155985 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 448 9 1 6 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(CC)C(C)C)cc3)oc2c1 nan
CHEMBL3943976 155985 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 448 9 1 6 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(CC)C(C)C)cc3)oc2c1 nan
71655255 97530 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 489 7 2 6 5.3 CCc1nnc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)[nH]1 10.1016/j.bmcl.2013.04.014
CHEMBL2391600 97530 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 489 7 2 6 5.3 CCc1nnc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)[nH]1 10.1016/j.bmcl.2013.04.014
156019826 184719 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 474 5 0 9 4.4 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(-n4cnnn4)cc3Cl)cs2)CC1 10.1016/j.bmcl.2019.126855
CHEMBL4645561 184719 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 474 5 0 9 4.4 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(-n4cnnn4)cc3Cl)cs2)CC1 10.1016/j.bmcl.2019.126855
122184144 129080 0 None 12 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 491 6 0 7 2.9 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598106 129080 0 None 12 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 491 6 0 7 2.9 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
87223807 187150 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 532 7 1 9 4.8 O=C1NC(=O)/C(=C/c2ccc(Oc3cc(OC4CCN(C(=O)OCc5ccccc5)CC4)ncn3)cc2)S1 10.1016/j.bmc.2021.116071
CHEMBL4751616 187150 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 532 7 1 9 4.8 O=C1NC(=O)/C(=C/c2ccc(Oc3cc(OC4CCN(C(=O)OCc5ccccc5)CC4)ncn3)cc2)S1 10.1016/j.bmc.2021.116071
67462505 151386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 8 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCCN4CCCCC4)c3)oc2c1 nan
CHEMBL3907852 151386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 8 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCCN4CCCCC4)c3)oc2c1 nan
54592031 155926 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 406 6 2 6 2.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)NC)cc3)oc2c1 nan
CHEMBL3943436 155926 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 406 6 2 6 2.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)NC)cc3)oc2c1 nan
71736417 140585 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 439 3 1 5 4.8 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C(N)=O)cc4F)ncc3o2)CC1 nan
CHEMBL3715408 140585 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 439 3 1 5 4.8 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C(N)=O)cc4F)ncc3o2)CC1 nan
156020078 184935 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 458 5 0 9 3.9 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(-n4cnnn4)cc3F)cs2)CC1 10.1016/j.bmcl.2019.126855
CHEMBL4648982 184935 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 458 5 0 9 3.9 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(-n4cnnn4)cc3F)cs2)CC1 10.1016/j.bmcl.2019.126855
122184143 129079 0 None -2 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 519 6 0 7 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598105 129079 0 None -2 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 519 6 0 7 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
54591409 157389 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 433 5 2 6 4.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCCCC4O)cc3)oc2c1 nan
CHEMBL3955267 157389 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 433 5 2 6 4.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCCCC4O)cc3)oc2c1 nan
54591408 167266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 391 5 1 5 4.8 CC[C@H]1C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)=NNC(=O)[C@@H]1C nan
CHEMBL4111982 167266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 391 5 1 5 4.8 CC[C@H]1C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)=NNC(=O)[C@@H]1C nan
89995642 154025 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 453 6 0 6 4.0 O=C(OCC1CCOCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3928529 154025 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 453 6 0 6 4.0 O=C(OCC1CCOCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
60155096 84165 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2cnc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
CHEMBL2086651 84165 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2cnc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
89995560 152067 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 465 5 1 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C(=O)O)nc3)cc2)C2CC2)CC1 nan
CHEMBL3913059 152067 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 465 5 1 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C(=O)O)nc3)cc2)C2CC2)CC1 nan
118711775 120800 0 None -11 2 Rat 7.0 pEC50 = 7.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326666 120800 0 None -11 2 Rat 7.0 pEC50 = 7.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
67462626 153088 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 461 7 1 7 3.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C)CC4)cc3)oc2c1 nan
CHEMBL3920966 153088 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 461 7 1 7 3.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C)CC4)cc3)oc2c1 nan
67464433 149991 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)N4CCCCC4)cc3)oc2c1 nan
CHEMBL3896383 149991 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)N4CCCCC4)cc3)oc2c1 nan
67450949 129061 0 None 8 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 454 6 0 7 3.5 Cc1nc(S(C)(=O)=O)ccc1O[C@H]1CC[C@H](OC2CCN(C(=O)OC(C)C)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598088 129061 0 None 8 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 454 6 0 7 3.5 Cc1nc(S(C)(=O)=O)ccc1O[C@H]1CC[C@H](OC2CCN(C(=O)OC(C)C)CC2)CC1 10.1016/j.bmcl.2015.04.102
54585807 68343 0 None 12 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 406 3 0 4 4.3 C[S+]([O-])c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771070 68343 0 None 12 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 406 3 0 4 4.3 C[S+]([O-])c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
127048495 147713 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 456 5 0 7 3.9 CC(C)COC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3822762 147713 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 456 5 0 7 3.9 CC(C)COC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
127048495 147713 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 456 5 0 7 3.9 CC(C)COC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmc.2017.06.014
CHEMBL3822762 147713 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 456 5 0 7 3.9 CC(C)COC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmc.2017.06.014
72945899 111394 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 499 6 0 6 4.7 Cc1cc2c(c(Oc3cccc(N(C)S(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104882 111394 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 499 6 0 6 4.7 Cc1cc2c(c(Oc3cccc(N(C)S(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
72945707 111403 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 471 6 1 6 4.3 CCN1C(=O)c2cc(C)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2C1=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104892 111403 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 471 6 1 6 4.3 CCN1C(=O)c2cc(C)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2C1=O 10.1016/j.bmcl.2013.11.053
71722055 122943 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358006 122943 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
118720416 122672 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.5 COC(=O)C1(Cc2ccccc2)COc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354788 122672 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.5 COC(=O)C1(Cc2ccccc2)COc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
66964510 117537 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260532 117537 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
73354931 96971 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccc(S(C)(=O)=O)cc3)cn1)C2 10.1016/j.bmcl.2013.04.006
CHEMBL2382409 96971 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccc(S(C)(=O)=O)cc3)cn1)C2 10.1016/j.bmcl.2013.04.006
73351961 96979 0 None 11 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382417 96979 0 None 11 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
46897577 111793 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 480 6 0 9 3.0 CCc1cnc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)nc1 10.1016/j.bmc.2014.01.028
CHEMBL3113622 111793 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 480 6 0 9 3.0 CCc1cnc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)nc1 10.1016/j.bmc.2014.01.028
24961799 68351 0 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccnc(C#N)n3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771079 68351 0 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccnc(C#N)n3)CC2)CC1 10.1016/j.bmcl.2010.12.086
25012524 68364 0 None -5 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 397 3 0 7 3.2 Cc1cc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
CHEMBL1771093 68364 0 None -5 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 397 3 0 7 3.2 Cc1cc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
49855246 122659 0 None -10 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(C)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
CHEMBL3354774 122659 0 None -10 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(C)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
118720412 122668 0 None -3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 431 5 0 5 5.0 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(Cl)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354784 122668 0 None -3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 431 5 0 5 5.0 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(Cl)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
71562723 110056 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 518 6 2 10 3.9 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084484 110056 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 518 6 2 10 3.9 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
53630395 68597 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 500 5 0 9 3.3 CN(CC1CCN(C(=O)OC(C)(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1 10.1016/j.bmcl.2011.03.007
CHEMBL1773279 68597 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 500 5 0 9 3.3 CN(CC1CCN(C(=O)OC(C)(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1 10.1016/j.bmcl.2011.03.007
25053188 183700 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 469 8 1 10 5.1 CCSc1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL461934 183700 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 469 8 1 10 5.1 CCSc1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
76324928 111689 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 570 5 0 7 6.4 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C(F)(F)F)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112981 111689 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 570 5 0 7 6.4 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C(F)(F)F)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
137645720 164367 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 505 6 1 10 3.3 CC(C)(C)OC(=O)N1CC2CC1CC2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4080761 164367 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 505 6 1 10 3.3 CC(C)(C)OC(=O)N1CC2CC1CC2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
66964662 117529 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 433 6 0 5 5.4 CCOC(=O)C(C)(Cc1ccccc1C)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260523 117529 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 433 6 0 5 5.4 CCOC(=O)C(C)(Cc1ccccc1C)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
67449879 129059 0 None -2 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 454 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598086 129059 0 None -2 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 454 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
67467956 166863 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 350 4 1 5 3.7 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cccn4C)oc3c2)[C@@H]1C nan
CHEMBL4108549 166863 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 350 4 1 5 3.7 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cccn4C)oc3c2)[C@@H]1C nan
118711219 120714 0 None -12 2 Rat 7.0 pEC50 = 7.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325852 120714 0 None -12 2 Rat 7.0 pEC50 = 7.0 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
90656489 117547 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 458 7 0 7 4.0 CCOC(=O)C(Cc1ccccc1)C1=NC=NC2C1N=CN2c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2014.03.023
CHEMBL3260543 117547 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 458 7 0 7 4.0 CCOC(=O)C(Cc1ccccc1)C1=NC=NC2C1N=CN2c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2014.03.023
57401198 77617 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 2 10 2.2 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1CO 10.1016/j.bmcl.2011.12.092
CHEMBL1951031 77617 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 2 10 2.2 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1CO 10.1016/j.bmcl.2011.12.092
118722584 122946 0 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 6 0 10 3.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(N=S(C)(C)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358009 122946 0 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 6 0 10 3.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(N=S(C)(C)=O)cc2F)cn1 10.1021/jm5011012
118300931 150260 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 513 6 1 5 4.3 CNS(=O)(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
CHEMBL3898585 150260 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 513 6 1 5 4.3 CNS(=O)(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
67464400 155579 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 361 5 1 4 4.8 CCCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3940831 155579 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 361 5 1 4 4.8 CCCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
76324299 110006 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 472 6 0 7 3.5 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084372 110006 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 472 6 0 7 3.5 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
76316927 110009 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 486 7 0 7 3.9 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084376 110009 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 486 7 0 7 3.9 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
51030336 84195 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 5 0 8 2.4 CC(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)[C@H](C)C1 10.1021/jm300310c
CHEMBL2086685 84195 0 None 4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 5 0 8 2.4 CC(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)[C@H](C)C1 10.1021/jm300310c
54590844 153025 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 449 6 1 7 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)OC(C)(C)C)cc3)oc2c1 nan
CHEMBL3920501 153025 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 449 6 1 7 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)OC(C)(C)C)cc3)oc2c1 nan
156012000 184123 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 440 5 0 9 3.7 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(-n4cnnn4)cc3)cs2)CC1 10.1016/j.bmcl.2019.126855
CHEMBL4637425 184123 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 440 5 0 9 3.7 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(-n4cnnn4)cc3)cs2)CC1 10.1016/j.bmcl.2019.126855
145955539 169384 0 None -8 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3c(F)cccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4169168 169384 0 None -8 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3c(F)cccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
89995715 154427 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 449 6 1 4 4.1 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C(N)=O)cc3)cc2)C2CC2)CC1 nan
CHEMBL3931574 154427 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 449 6 1 4 4.1 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C(N)=O)cc3)cc2)C2CC2)CC1 nan
54591024 157969 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 312 2 1 5 2.7 CC1CC(=O)NN=C1c1ccc2nc(N3CCCCC3)oc2c1 nan
CHEMBL3959792 157969 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 312 2 1 5 2.7 CC1CC(=O)NN=C1c1ccc2nc(N3CCCCC3)oc2c1 nan
122194337 130771 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
CHEMBL3629478 130771 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
54590932 158482 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 363 5 1 5 4.1 CCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1 nan
CHEMBL3964304 158482 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 363 5 1 5 4.1 CCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1 nan
67466152 158967 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCCC4)cc3)oc2c1 nan
CHEMBL3968428 158967 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCCC4)cc3)oc2c1 nan
67465379 157618 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 1 5 3.4 COc1ccccc1-c1nc2ccc(C3=NNC(=O)CC3C)cc2o1 nan
CHEMBL3957066 157618 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 1 5 3.4 COc1ccccc1-c1nc2ccc(C3=NNC(=O)CC3C)cc2o1 nan
60155097 84166 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
CHEMBL2086652 84166 0 None -2 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
57403665 77639 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 515 8 1 10 3.3 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1OC(F)F 10.1016/j.bmcl.2011.12.092
CHEMBL1951115 77639 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 515 8 1 10 3.3 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1OC(F)F 10.1016/j.bmcl.2011.12.092
62706850 83078 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 7 3.2 COc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058667 83078 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 7 3.2 COc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
118300930 155828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 499 5 1 5 4.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(N)(=O)=O)cc3)cc2)C2CC2)CC1 nan
CHEMBL3942809 155828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 499 5 1 5 4.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(N)(=O)=O)cc3)cc2)C2CC2)CC1 nan
54582694 69002 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 6 1 8 2.1 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(O)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778252 69002 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 6 1 8 2.1 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(O)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
60155457 84190 0 None -18 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 389 4 0 7 2.6 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3F)cn2)CC1 10.1021/jm300310c
CHEMBL2086679 84190 0 None -18 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 389 4 0 7 2.6 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3F)cn2)CC1 10.1021/jm300310c
11283457 68606 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 501 4 0 9 3.6 Cc1nc(OC2CCN(C(=O)OC(C)(C)C)CC2)c2c(C)nn(-c3ccc(S(C)(=O)=O)cc3)c2n1 10.1016/j.bmcl.2011.03.007
CHEMBL1773289 68606 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 501 4 0 9 3.6 Cc1nc(OC2CCN(C(=O)OC(C)(C)C)CC2)c2c(C)nn(-c3ccc(S(C)(=O)=O)cc3)c2n1 10.1016/j.bmcl.2011.03.007
54586777 68348 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771076 68348 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
68209221 153454 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 502 7 1 6 6.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4C(C)(C)CCCC4(C)C)c3)oc2c1 nan
CHEMBL3923800 153454 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 502 7 1 6 6.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4C(C)(C)CCCC4(C)C)c3)oc2c1 nan
67464383 167298 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 365 4 1 4 4.5 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(F)cc4)oc3c2)[C@@H]1C nan
CHEMBL4112277 167298 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 365 4 1 4 4.5 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(F)cc4)oc3c2)[C@@H]1C nan
67450521 129066 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598093 129066 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
62706849 83077 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 380 7 1 6 3.7 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058666 83077 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 380 7 1 6 3.7 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
89995540 151898 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 514 5 1 7 4.3 CN(C)C(=O)Nc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)ns1 nan
CHEMBL3911907 151898 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 514 5 1 7 4.3 CN(C)C(=O)Nc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)ns1 nan
54591264 155329 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 547 7 1 8 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(=O)OC(C)(C)C)CC4)cc3)oc2c1 nan
CHEMBL3938721 155329 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 547 7 1 8 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(=O)OC(C)(C)C)CC4)cc3)oc2c1 nan
67464445 159147 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OC(C)CN4CCCCC4)c3)oc2c1 nan
CHEMBL3970172 159147 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OC(C)CN4CCCCC4)c3)oc2c1 nan
54596144 129067 0 None -3 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 441 6 0 8 2.6 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598094 129067 0 None -3 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 441 6 0 8 2.6 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
71736723 141108 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 460 4 0 6 4.8 CC(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc3o2)CC1 nan
CHEMBL3717176 141108 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 460 4 0 6 4.8 CC(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc3o2)CC1 nan
58190324 122949 0 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 548 6 0 9 2.6 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358012 122949 0 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 548 6 0 9 2.6 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
70693586 79845 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 483 6 0 8 3.0 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2nc3cc(F)ccc3s2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010850 79845 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 483 6 0 8 3.0 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2nc3cc(F)ccc3s2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
139436992 182594 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 466 7 0 8 2.2 COC(=O)C1CN(c2ccc(N3CC[C@@H](Oc4ccc(OCC(F)(F)F)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
CHEMBL4584670 182594 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 466 7 0 8 2.2 COC(=O)C1CN(c2ccc(N3CC[C@@H](Oc4ccc(OCC(F)(F)F)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
71116113 130520 0 None -1 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 477 10 0 7 3.6 CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(COC)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
CHEMBL3622177 130520 0 None -1 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 477 10 0 7 3.6 CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(COC)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
24899742 89296 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 544 5 0 8 4.6 CS(=O)(=O)c1ccc(N2CCc3c(OC4CCN(C(=S)Sc5ccccc5)CC4)ncnc32)c(F)c1 10.1021/jm301404a
CHEMBL2177763 89296 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 544 5 0 8 4.6 CS(=O)(=O)c1ccc(N2CCc3c(OC4CCN(C(=S)Sc5ccccc5)CC4)ncnc32)c(F)c1 10.1021/jm301404a
53321124 65333 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 396 5 1 3 3.9 CC(CNC(=O)Cc1c(F)cccc1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684033 65333 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 396 5 1 3 3.9 CC(CNC(=O)Cc1c(F)cccc1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
76310397 111728 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 522 6 0 7 5.9 Cc1cc(-c2nc(C3CC3)no2)cc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)n1 10.1016/j.bmcl.2013.12.127
CHEMBL3113205 111728 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 522 6 0 7 5.9 Cc1cc(-c2nc(C3CC3)no2)cc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)n1 10.1016/j.bmcl.2013.12.127
57394950 77640 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 474 6 1 10 2.6 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C#N 10.1016/j.bmcl.2011.12.092
CHEMBL1951116 77640 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 474 6 1 10 2.6 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C#N 10.1016/j.bmcl.2011.12.092
76324976 111796 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 450 5 0 5 3.8 CC(C)(C)OC(=O)N1CCC(CCCC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113625 111796 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 450 5 0 5 3.8 CC(C)(C)OC(=O)N1CCC(CCCC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
51030053 84191 1 None -23 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086680 84191 1 None -23 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
51030053 84191 1 None -23 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1021/jm300310c
CHEMBL2086680 84191 1 None -23 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1021/jm300310c
54586987 68603 0 None -16 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 471 4 0 8 3.4 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773286 68603 0 None -16 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 471 4 0 8 3.4 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
67462477 155774 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)(C)CN4CCOCC4)cc3)oc2c1 nan
CHEMBL3942311 155774 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)(C)CN4CCOCC4)cc3)oc2c1 nan
67461228 158159 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 2 1 5 3.4 CC1CC(=O)NN=C1c1ccc2nc(-c3cccs3)oc2c1 nan
CHEMBL3961465 158159 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 2 1 5 3.4 CC1CC(=O)NN=C1c1ccc2nc(-c3cccs3)oc2c1 nan
67464365 159120 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 349 4 1 5 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)cc3)oc2c1 nan
CHEMBL3969881 159120 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 349 4 1 5 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)cc3)oc2c1 nan
25052970 179767 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 449 7 1 10 2.3 CCOC(=O)C1CCN(c2ncnc(Nc3ccc(S(C)(=O)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL451797 179767 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 449 7 1 10 2.3 CCOC(=O)C1CCN(c2ncnc(Nc3ccc(S(C)(=O)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
68299308 120326 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 508 6 0 9 4.2 CCc1cnc(N2CCC(N(C)c3ncnc4c(-c5ccc(S(C)(=O)=O)cc5)csc34)CC2)nc1 10.1016/j.bmcl.2014.07.020
CHEMBL3321827 120326 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 508 6 0 9 4.2 CCc1cnc(N2CCC(N(C)c3ncnc4c(-c5ccc(S(C)(=O)=O)cc5)csc34)CC2)nc1 10.1016/j.bmcl.2014.07.020
118709767 120332 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 508 6 0 8 3.4 CC(C)S(=O)(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321834 120332 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 508 6 0 8 3.4 CC(C)S(=O)(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
66964174 117522 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 329 4 0 5 3.7 CCOC(=O)C(C)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260514 117522 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 329 4 0 5 3.7 CCOC(=O)C(C)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
46884935 14752 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 497 9 0 7 2.4 CCN(CC)S(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1090558 14752 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 497 9 0 7 2.4 CCN(CC)S(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
46885169 15189 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 468 8 0 7 2.6 CCS(=O)(=O)N1CCN(c2ccc(OCCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1093452 15189 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 468 8 0 7 2.6 CCS(=O)(=O)N1CCN(c2ccc(OCCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
54591019 155968 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 403 4 1 5 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(F)(F)F)cc3)oc2c1 nan
CHEMBL3943781 155968 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 403 4 1 5 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(F)(F)F)cc3)oc2c1 nan
71736413 141061 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 471 4 1 6 5.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(NS(C)(=O)=O)cc4)ncc3o2)CC1 nan
CHEMBL3717009 141061 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 471 4 1 6 5.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(NS(C)(=O)=O)cc4)ncc3o2)CC1 nan
72945519 111401 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 443 5 2 6 3.5 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)NC2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104890 111401 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 443 5 2 6 3.5 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)NC2=O 10.1016/j.bmcl.2013.11.053
71545699 93021 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 504 5 0 8 3.8 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312518 93021 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 504 5 0 8 3.8 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
62707005 83083 0 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 400 7 1 7 4.3 CC(C)c1nsc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)n1 10.1016/j.bmcl.2012.05.117
CHEMBL2058672 83083 0 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 400 7 1 7 4.3 CC(C)c1nsc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)n1 10.1016/j.bmcl.2012.05.117
68240486 130773 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 2.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(S(=O)(=O)C1CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629480 130773 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 2.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(S(=O)(=O)C1CC1)C2 10.1016/j.bmcl.2015.09.047
68211781 117669 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 544 9 1 7 3.6 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCCO)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261138 117669 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 544 9 1 7 3.6 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCCO)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
70687331 79827 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 486 6 0 4 3.9 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1F)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010832 79827 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 486 6 0 4 3.9 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1F)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
68209375 160792 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 7 1 6 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCOC)cc3)oc2c1 nan
CHEMBL3984128 160792 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 7 1 6 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCOC)cc3)oc2c1 nan
145968330 171808 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 461 8 0 6 4.4 CCc1cnc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)c(F)c2)C3)nc1 10.1016/j.bmc.2018.02.032
CHEMBL4226130 171808 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 461 8 0 6 4.4 CCc1cnc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)c(F)c2)C3)nc1 10.1016/j.bmc.2018.02.032
62706518 83015 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CC3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058403 83015 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CC3)CC1 10.1016/j.bmcl.2012.05.117
118711791 120817 0 None -5 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 8 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3(F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326682 120817 0 None -5 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 8 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3(F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
54583401 68009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(OC2C3COC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766083 68009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(OC2C3COC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
73388222 155107 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 395 5 0 5 4.1 C=C(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3937017 155107 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 395 5 0 5 4.1 C=C(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
54591263 159455 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 11 1 6 5.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(CC(C)C)CC(C)C)cc3)oc2c1 nan
CHEMBL3972704 159455 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 11 1 6 5.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(CC(C)C)CC(C)C)cc3)oc2c1 nan
118720413 122669 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 461 5 0 7 3.4 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(S(C)(=O)=O)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354785 122669 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 461 5 0 7 3.4 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(S(C)(=O)=O)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
56960929 189570 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 5 1 9 4.4 CC(C)(C)OC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4790521 189570 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 5 1 9 4.4 CC(C)(C)OC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
58017028 89304 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 506 4 0 8 3.8 Cc1nc(OC2CCN(C(=O)OC(C)(C)C)CC2)c2c(n1)N(c1ccc(S(C)(=O)=O)cc1F)CC2 10.1021/jm301404a
CHEMBL2177772 89304 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 506 4 0 8 3.8 Cc1nc(OC2CCN(C(=O)OC(C)(C)C)CC2)c2c(n1)N(c1ccc(S(C)(=O)=O)cc1F)CC2 10.1021/jm301404a
24897242 89313 1 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
CHEMBL2177781 89313 1 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
58017018 89828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 461 5 0 9 2.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cn2)CC1 10.1021/jm301404a
CHEMBL2181681 89828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 461 5 0 9 2.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cn2)CC1 10.1021/jm301404a
24899748 89298 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 498 6 0 8 2.3 CC(C)S(=O)(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177765 89298 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 498 6 0 8 2.3 CC(C)S(=O)(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
90666915 116238 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)O[C@H]2CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220243 116238 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)O[C@H]2CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
145984643 173182 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 588 6 0 6 6.1 C[C@H](OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1016/j.bmcl.2018.08.010
CHEMBL4276952 173182 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 588 6 0 6 6.1 C[C@H](OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1016/j.bmcl.2018.08.010
118711782 120809 0 None -5 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326674 120809 0 None -5 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
68209624 160475 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccncc4)c3)oc2c1 nan
CHEMBL3981413 160475 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccncc4)c3)oc2c1 nan
89995535 157591 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 505 5 0 5 5.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(N4CCOCC4)cc3)cc2)C2CC2)CC1 nan
CHEMBL3956800 157591 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 505 5 0 5 5.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(N4CCOCC4)cc3)cc2)C2CC2)CC1 nan
90000583 158410 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 6 3.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cncn3)cc2)C2CC2)CC1 nan
CHEMBL3963782 158410 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 6 3.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cncn3)cc2)C2CC2)CC1 nan
54591338 166668 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 365 4 1 5 4.6 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cc(C)oc4C)oc3c2)[C@@H]1C nan
CHEMBL4106877 166668 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 365 4 1 5 4.6 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cc(C)oc4C)oc3c2)[C@@H]1C nan
140253895 173549 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 534 6 0 6 5.6 CC(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4283838 173549 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 534 6 0 6 5.6 CC(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
68040003 130770 0 None -8 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 484 5 0 8 4.1 Cc1c(Oc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629477 130770 0 None -8 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 484 5 0 8 4.1 Cc1c(Oc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
89995561 153319 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 445 6 0 5 4.7 O=C(OCc1ccccc1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3922712 153319 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 445 6 0 5 4.7 O=C(OCc1ccccc1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
56591900 165955 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 490 4 1 8 4.6 CC(C)(C)OC(=O)N1CCC(c2coc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL4098382 165955 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 490 4 1 8 4.6 CC(C)(C)OC(=O)N1CCC(c2coc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
71736724 140758 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 472 4 0 6 4.9 CC1(OC(=O)N2CCC(c3cc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc4o3)CC2)CC1 nan
CHEMBL3716002 140758 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 472 4 0 6 4.9 CC1(OC(=O)N2CCC(c3cc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc4o3)CC2)CC1 nan
53326341 65320 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 414 5 1 3 4.0 CC(CNC(=O)Cc1c(F)ccc(F)c1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1683944 65320 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 414 5 1 3 4.0 CC(CNC(=O)Cc1c(F)ccc(F)c1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
67449861 129060 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 440 6 0 7 3.2 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598087 129060 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 440 6 0 7 3.2 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
54585809 68363 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 467 4 0 5 4.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C(F)(F)F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771092 68363 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 467 4 0 5 4.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C(F)(F)F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
68022035 147825 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 462 5 0 8 3.7 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
CHEMBL3824187 147825 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 462 5 0 8 3.7 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
140251501 171770 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 453 7 0 5 4.6 CC1(OC(=O)N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)c(F)c2)C3)CC1 10.1016/j.bmc.2018.02.032
CHEMBL4225663 171770 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 453 7 0 5 4.6 CC1(OC(=O)N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)c(F)c2)C3)CC1 10.1016/j.bmc.2018.02.032
68022035 147825 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 462 5 0 8 3.7 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL3824187 147825 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 462 5 0 8 3.7 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
137661403 166053 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 490 6 1 8 4.1 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(Cl)c1 10.1016/j.bmc.2017.06.014
CHEMBL4099323 166053 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 490 6 1 8 4.1 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(Cl)c1 10.1016/j.bmc.2017.06.014
71655093 97462 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 471 7 1 7 4.7 CCOC(=O)c1cc(C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
CHEMBL2391429 97462 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 471 7 1 7 4.7 CCOC(=O)c1cc(C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
72945708 111404 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 485 6 1 6 4.6 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104893 111404 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 485 6 1 6 4.6 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
145955539 169384 0 None 8 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3c(F)cccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4169168 169384 0 None 8 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3c(F)cccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
155534233 178722 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 463 5 1 7 4.6 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4470443 178722 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 463 5 1 7 4.6 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
71547008 92960 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 508 4 0 10 3.8 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312159 92960 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 508 4 0 10 3.8 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
118711783 120810 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326675 120810 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711212 120707 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325845 120707 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
54596144 129067 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 441 6 0 8 2.6 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598094 129067 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 441 6 0 8 2.6 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
66574514 120801 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2015.04.102
CHEMBL3326667 120801 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2015.04.102
66574514 120801 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326667 120801 0 None 12 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
46885171 14988 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR119 receptor by cell based cAMP assayAgonist activity at GPR119 receptor by cell based cAMP assay
ChEMBL 475 7 1 11 3.9 O=[N+]([O-])c1c(Nc2ccc(-n3cncn3)cc2)ncnc1N1CCC(Sc2ccccn2)CC1 10.1021/jm301404a
CHEMBL1092240 14988 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR119 receptor by cell based cAMP assayAgonist activity at GPR119 receptor by cell based cAMP assay
ChEMBL 475 7 1 11 3.9 O=[N+]([O-])c1c(Nc2ccc(-n3cncn3)cc2)ncnc1N1CCC(Sc2ccccn2)CC1 10.1021/jm301404a
71655094 97464 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 497 8 1 7 5.3 CCOC(=O)c1cc(C2CC2)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
CHEMBL2391430 97464 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 497 8 1 7 5.3 CCOC(=O)c1cc(C2CC2)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
76332169 111687 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 548 7 0 7 6.5 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(C4CC4)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112979 111687 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 548 7 0 7 6.5 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(C4CC4)n3)cc21 10.1016/j.bmcl.2013.12.127
54586563 69003 0 None 5 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 448 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778253 69003 0 None 5 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 448 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
71545380 93027 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2CCC2)c1C 10.1021/jm301626p
CHEMBL2312523 93027 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2CCC2)c1C 10.1021/jm301626p
66964756 117534 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3cccc(Cl)c3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260528 117534 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3cccc(Cl)c3)cnn12 10.1016/j.bmcl.2014.03.023
46885171 14988 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor by cAMP mobilization assayAgonist activity at human GPR119 receptor by cAMP mobilization assay
ChEMBL 475 7 1 11 3.9 O=[N+]([O-])c1c(Nc2ccc(-n3cncn3)cc2)ncnc1N1CCC(Sc2ccccn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1092240 14988 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor by cAMP mobilization assayAgonist activity at human GPR119 receptor by cAMP mobilization assay
ChEMBL 475 7 1 11 3.9 O=[N+]([O-])c1c(Nc2ccc(-n3cncn3)cc2)ncnc1N1CCC(Sc2ccccn2)CC1 10.1016/j.bmcl.2010.02.083
56960790 188738 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 5 1 9 4.4 CC(C)(C)OC(=O)N1CCC(Oc2cc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4779985 188738 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 5 1 9 4.4 CC(C)(C)OC(=O)N1CCC(Oc2cc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)ncn2)CC1 10.1016/j.bmc.2021.116071
66964682 117516 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 501 7 0 7 4.5 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(S(C)(=O)=O)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260507 117516 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 501 7 0 7 4.5 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(S(C)(=O)=O)cc3)cnn12 10.1016/j.bmcl.2014.03.023
46884822 15112 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 454 7 0 7 2.2 CCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1092895 15112 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 454 7 0 7 2.2 CCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
67466215 153118 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 336 2 1 5 2.6 O=C1CC(C2CC2)C(N2CCc3nc(-c4ccccc4)oc3C2)=NN1 nan
CHEMBL3921229 153118 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 336 2 1 5 2.6 O=C1CC(C2CC2)C(N2CCc3nc(-c4ccccc4)oc3C2)=NN1 nan
76309729 110000 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 398 5 0 7 3.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
CHEMBL3084366 110000 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 398 5 0 7 3.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
23649212 77608 2 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951022 77608 2 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
70685174 79828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 486 6 0 4 3.9 CN(C(=O)Cc1ccc(S(C)(=O)=O)c(F)c1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010833 79828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 486 6 0 4 3.9 CN(C(=O)Cc1ccc(S(C)(=O)=O)c(F)c1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
54580904 68359 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 433 4 0 5 4.3 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771088 68359 0 None -2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 433 4 0 5 4.3 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
60155366 84185 0 None -8 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 487 5 0 9 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm300310c
CHEMBL2086673 84185 0 None -8 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 487 5 0 9 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm300310c
118300927 158588 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 451 5 0 5 4.8 COc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
CHEMBL3965234 158588 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 451 5 0 5 4.8 COc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
145974170 171372 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 373 8 0 3 5.1 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4215690 171372 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 373 8 0 3 5.1 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
57397676 77606 0 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 416 6 0 8 3.7 COc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
CHEMBL1951020 77606 0 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 416 6 0 8 3.7 COc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
54585807 68343 0 None -12 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 406 3 0 4 4.3 C[S+]([O-])c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771070 68343 0 None -12 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 406 3 0 4 4.3 C[S+]([O-])c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
54590930 159320 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 4 4.0 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(Cl)cc3)oc2c1 nan
CHEMBL3971612 159320 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 4 4.0 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(Cl)cc3)oc2c1 nan
118711210 120704 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 467 6 1 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325842 120704 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 467 6 1 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
11691227 77638 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 465 6 2 10 2.4 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1O 10.1016/j.bmcl.2011.12.092
CHEMBL1951114 77638 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 465 6 2 10 2.4 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1O 10.1016/j.bmcl.2011.12.092
118711214 120709 0 None -14 2 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 493 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C#N)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325847 120709 0 None -14 2 Rat 5.9 pEC50 = 5.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 493 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C#N)CC2)c1F 10.1016/j.bmcl.2014.06.071
54591022 149184 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 281 2 1 5 2.7 O=C1CCC(c2ccc3nc(-c4ccco4)oc3c2)=NN1 nan
CHEMBL3889761 149184 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 281 2 1 5 2.7 O=C1CCC(c2ccc3nc(-c4ccco4)oc3c2)=NN1 nan
118722573 122933 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 498 6 0 10 2.6 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm5011012
CHEMBL3357997 122933 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 498 6 0 10 2.6 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm5011012
54591406 167164 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 324 2 1 5 2.6 CC[C@@H]1CC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
CHEMBL4111176 167164 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 324 2 1 5 2.6 CC[C@@H]1CC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
66556631 93754 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 498 6 0 7 4.3 CS(=O)(=O)c1ccc([C@H]2CC[C@H](OCC3CCN(c4ncc(C(F)(F)F)cn4)CC3)CC2)nc1 10.1021/ml300399u
CHEMBL2323594 93754 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 498 6 0 7 4.3 CS(=O)(=O)c1ccc([C@H]2CC[C@H](OCC3CCN(c4ncc(C(F)(F)F)cn4)CC3)CC2)nc1 10.1021/ml300399u
54591335 151185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 404 4 1 6 3.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N4CCOCC4)cc3)oc2c1 nan
CHEMBL3906089 151185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 404 4 1 6 3.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N4CCOCC4)cc3)oc2c1 nan
67464602 167406 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 353 4 1 5 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cccs4)oc3c2)[C@@H]1C nan
CHEMBL4113080 167406 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 353 4 1 5 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cccs4)oc3c2)[C@@H]1C nan
17993542 156893 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 374 2 1 5 4.1 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(Cl)nc3Cl)oc2c1 nan
CHEMBL3951146 156893 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 374 2 1 5 4.1 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(Cl)nc3Cl)oc2c1 nan
70689385 79832 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 459 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010838 79832 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 459 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2011.10.033
54591869 150254 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 501 4 1 7 4.0 CC(C)(C)OC(=O)N1CCN(Cc2ccc(-c3nc4ccc(C5=NNC(=O)C6CC56)cc4o3)cc2)CC1 nan
CHEMBL3898551 150254 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 501 4 1 7 4.0 CC(C)(C)OC(=O)N1CCN(Cc2ccc(-c3nc4ccc(C5=NNC(=O)C6CC56)cc4o3)cc2)CC1 nan
118720421 122677 0 None -1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 468 4 0 6 4.6 COC(=O)[C@@]1(Cc2cccc(F)c2)N=Cc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354793 122677 0 None -1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 468 4 0 6 4.6 COC(=O)[C@@]1(Cc2cccc(F)c2)N=Cc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
89995549 155396 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 414 4 2 7 2.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(N3C=NNN3)cc2)C2CC2)CC1 nan
CHEMBL3939288 155396 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 414 4 2 7 2.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(N3C=NNN3)cc2)C2CC2)CC1 nan
60155096 84165 0 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2cnc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
CHEMBL2086651 84165 0 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2cnc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
53491715 129068 0 None -5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 453 6 0 8 2.7 CC1(OC(=O)N2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598095 129068 0 None -5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 453 6 0 8 2.7 CC1(OC(=O)N2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)CC1 10.1016/j.bmcl.2015.04.102
118711215 120710 0 None -6 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 500 7 0 9 3.2 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325848 120710 0 None -6 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 500 7 0 9 3.2 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
53319831 65339 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 416 6 1 3 3.5 CC1(OC(=O)N2CCC([C@@H](F)CNC(=O)Cc3c(F)ccc(F)c3F)CC2)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684040 65339 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 416 6 1 3 3.5 CC1(OC(=O)N2CCC([C@@H](F)CNC(=O)Cc3c(F)ccc(F)c3F)CC2)CC1 10.1016/j.bmcl.2011.01.088
122184144 129080 0 None -12 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 491 6 0 7 2.9 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598106 129080 0 None -12 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 491 6 0 7 2.9 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
155517437 176952 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 5 1 7 4.4 Cc1c(Nc2ccc(S(C)(=O)=O)cc2)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4444597 176952 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 5 1 7 4.4 Cc1c(Nc2ccc(S(C)(=O)=O)cc2)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
62706851 83079 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 7 1 8 2.9 COC(=O)c1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058668 83079 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 7 1 8 2.9 COC(=O)c1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
118300923 151272 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 488 5 0 7 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cnc(-c4ccncn4)c3)cc2)C2CC2)CC1 nan
CHEMBL3906852 151272 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 488 5 0 7 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cnc(-c4ccncn4)c3)cc2)C2CC2)CC1 nan
53492467 129055 0 None -5 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598082 129055 0 None -5 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
16036825 68007 0 None 7 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
CHEMBL1766081 68007 0 None 7 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
122184147 129086 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
CHEMBL3598112 129086 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
11271133 68609 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 460 5 0 9 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)noc23)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773294 68609 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 460 5 0 9 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)noc23)CC1 10.1016/j.bmcl.2011.03.007
54587813 68369 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771098 68369 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
89677943 192237 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 501 5 0 8 3.8 CCN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
CHEMBL4861760 192237 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 501 5 0 8 3.8 CCN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
127048493 147820 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 485 6 1 6 4.7 CCCNC(=O)c1cc(F)c(-c2cc3cnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmcl.2016.06.050
CHEMBL3824111 147820 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 485 6 1 6 4.7 CCCNC(=O)c1cc(F)c(-c2cc3cnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmcl.2016.06.050
76683708 171864 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 437 6 0 5 4.7 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4227018 171864 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 437 6 0 5 4.7 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
57405092 164844 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 461 5 0 7 4.3 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ccc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4086175 164844 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 461 5 0 7 4.3 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ccc43)CC2)nc1 10.1016/j.bmc.2017.06.014
145973091 171482 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 425 8 0 5 4.7 CC(C)(C)OC(=O)N1CCC(CCCCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
CHEMBL4217229 171482 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 425 8 0 5 4.7 CC(C)(C)OC(=O)N1CCC(CCCCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
54589230 117658 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 536 6 0 6 4.5 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ncc(C(F)(F)F)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261127 117658 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 536 6 0 6 4.5 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ncc(C(F)(F)F)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
71531541 147263 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assay
ChEMBL 395 7 1 7 3.4 CCc1cnc(N2CCC(C(C)CCNc3cc4c(cn3)C(=O)CO4)CC2)nc1 10.1021/acs.jmedchem.5b01198
CHEMBL3809686 147263 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assay
ChEMBL 395 7 1 7 3.4 CCc1cnc(N2CCC(C(C)CCNc3cc4c(cn3)C(=O)CO4)CC2)nc1 10.1021/acs.jmedchem.5b01198
51030987 84201 0 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2noc(C3CC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086691 84201 0 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2noc(C3CC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
118720419 122675 0 None -4 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 470 4 1 6 4.3 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354791 122675 0 None -4 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 470 4 1 6 4.3 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
118711795 120821 0 None 7 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)(C)F)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326686 120821 0 None 7 2 Human 7.9 pEC50 = 7.9 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)(C)F)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711778 120805 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 548 6 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326670 120805 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 548 6 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
71562845 110053 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 519 6 1 10 3.8 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084480 110053 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 519 6 1 10 3.8 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
53630450 68869 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 485 5 0 9 3.1 CS(=O)(=O)c1ccc(-n2ncc3c(OC4CCN(C(=O)OC5CCCC5)CC4)ncnc32)cc1 10.1016/j.bmcl.2011.03.007
CHEMBL1775174 68869 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 485 5 0 9 3.1 CS(=O)(=O)c1ccc(-n2ncc3c(OC4CCN(C(=O)OC5CCCC5)CC4)ncnc32)cc1 10.1016/j.bmcl.2011.03.007
86694586 140930 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 470 3 0 6 5.2 CC(C)(C)OC(=O)N1CCC(C)(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc3o2)CC1 nan
CHEMBL3716569 140930 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 470 3 0 6 5.2 CC(C)(C)OC(=O)N1CCC(C)(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc3o2)CC1 nan
118709768 120335 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 490 5 0 7 4.0 CC(C)C(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4F)csc23)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321838 120335 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 490 5 0 7 4.0 CC(C)C(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4F)csc23)CC1 10.1016/j.bmcl.2014.07.020
76317599 111694 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4noc(C5CC5)n4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112986 111694 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4noc(C5CC5)n4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
71717312 92912 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 489 4 0 9 4.3 Cc1c(Oc2ccc(-n3cncn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2311545 92912 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 489 4 0 9 4.3 Cc1c(Oc2ccc(-n3cncn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
66964600 117527 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 433 6 0 5 5.4 CCOC(=O)C(C)(Cc1ccc(C)cc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260521 117527 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 433 6 0 5 5.4 CCOC(=O)C(C)(Cc1ccc(C)cc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
70695705 79842 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 477 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)cn2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010848 79842 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 477 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)cn2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
68240419 130774 0 None -5 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629481 130774 0 None -5 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
53235503 110022 0 None -46 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 473 6 1 7 3.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084389 110022 0 None -46 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 473 6 1 7 3.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
58190330 122947 0 None -7 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 562 7 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358010 122947 0 None -7 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 562 7 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
57392379 77610 0 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1cc(S(C)(=O)=O)ncc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951024 77610 0 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1cc(S(C)(=O)=O)ncc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
132585244 189143 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 586 8 1 13 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3nc(-c4ccccc4)no3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4784857 189143 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 586 8 1 13 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3nc(-c4ccccc4)no3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
4400062 117515 15 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 457 6 0 5 5.7 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260506 117515 15 None -1 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 457 6 0 5 5.7 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
54581957 68337 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 344 2 0 3 4.6 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771064 68337 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 344 2 0 3 4.6 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
145983474 172229 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 525 5 2 10 3.9 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4239203 172229 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 525 5 2 10 3.9 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4)ncnc13)C2 10.1016/j.bmc.2018.06.035
76335866 111795 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 436 6 0 5 4.3 CC(C)(C)OC(=O)N1CCC(CCCCN2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113624 111795 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 436 6 0 5 4.3 CC(C)(C)OC(=O)N1CCC(CCCCN2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
58114293 90446 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR119 in human HEK293 cells by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells by beta-lactamase reporter gene assay
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
CHEMBL2204982 90446 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR119 in human HEK293 cells by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells by beta-lactamase reporter gene assay
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
67462327 150377 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 337 3 1 5 4.4 CCC1SC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3899479 150377 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 337 3 1 5 4.4 CCC1SC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
162650112 186952 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 538 7 1 12 -0.0 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(F)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4749117 186952 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 538 7 1 12 -0.0 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(F)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
57393406 77368 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 480 7 1 11 2.3 CC(C)OC(=O)N1CCC(Oc2cc(Nc3ccc(S(C)(=O)=O)nc3[N+](=O)[O-])ncn2)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1949688 77368 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 480 7 1 11 2.3 CC(C)OC(=O)N1CCC(Oc2cc(Nc3ccc(S(C)(=O)=O)nc3[N+](=O)[O-])ncn2)CC1 10.1016/j.bmcl.2011.12.092
67460937 156693 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 2 6 2.3 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N)nc3)oc2c1 nan
CHEMBL3949435 156693 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 2 6 2.3 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N)nc3)oc2c1 nan
56960789 188946 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 470 5 1 9 3.5 COC(=O)N1CCC(Oc2ncnc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)c2C)CC1 10.1016/j.bmc.2021.116071
CHEMBL4782568 188946 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 470 5 1 9 3.5 COC(=O)N1CCC(Oc2ncnc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)c2C)CC1 10.1016/j.bmc.2021.116071
71081343 173944 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 499 4 0 5 5.8 CC(C)S(=O)(=O)Cc1ccc(-c2ccc3c(c2)CCC2(CCN(C(=O)OC(C)(C)C)CC2)O3)cc1 10.1016/j.bmcl.2018.08.010
CHEMBL4291039 173944 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 499 4 0 5 5.8 CC(C)S(=O)(=O)Cc1ccc(-c2ccc3c(c2)CCC2(CCN(C(=O)OC(C)(C)C)CC2)O3)cc1 10.1016/j.bmcl.2018.08.010
54581959 68350 0 None -1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cnccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771078 68350 0 None -1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cnccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
67466315 149420 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)cc3F)oc2c1 nan
CHEMBL3891691 149420 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)cc3F)oc2c1 nan
67462730 166803 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 381 4 1 4 5.0 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(Cl)cc4)oc3c2)[C@@H]1C nan
CHEMBL4108022 166803 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 381 4 1 4 5.0 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(Cl)cc4)oc3c2)[C@@H]1C nan
118711211 120705 0 None -6 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 468 6 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325843 120705 0 None -6 2 Rat 6.9 pEC50 = 6.9 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 468 6 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
67464513 151050 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 5 1 7 5.4 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCC4CCN(C(=O)OC(C)(C)C)CC4)c3)oc2c1 nan
CHEMBL3904956 151050 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 5 1 7 5.4 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCC4CCN(C(=O)OC(C)(C)C)CC4)c3)oc2c1 nan
71546202 93014 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 453 4 0 8 4.1 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312511 93014 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 453 4 0 8 4.1 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71546853 93016 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 465 3 0 7 4.7 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312513 93016 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 465 3 0 7 4.7 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
118722570 122930 0 None -6 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3357994 122930 0 None -6 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
71545536 93030 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.4 CC[C@@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
CHEMBL2312526 93030 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.4 CC[C@@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
62706193 83003 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 436 7 1 5 4.6 CC(C)(C)OC(=O)N1CCC(CCCCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058390 83003 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 436 7 1 5 4.6 CC(C)(C)OC(=O)N1CCC(CCCCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
76331519 110011 0 None -5 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 506 6 0 8 4.8 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(Cl)s2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084378 110011 0 None -5 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 506 6 0 8 4.8 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(Cl)s2)c1C 10.1016/j.bmcl.2011.04.035
67462513 158564 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 431 6 1 5 5.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCCCC4)cc3)oc2c1 nan
CHEMBL3965027 158564 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 431 6 1 5 5.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCCCC4)cc3)oc2c1 nan
162663951 188930 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 586 8 1 13 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3noc(-c4ccccc4)n3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4782382 188930 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 586 8 1 13 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3noc(-c4ccccc4)n3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
145986191 172407 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 464 4 2 9 4.0 CC(C)(C)OC(=O)N1CCC(Nc2ncnc3c(Nc4ccc(C#N)cc4F)ncnc23)CC1 10.1016/j.bmc.2018.06.035
CHEMBL4243608 172407 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 464 4 2 9 4.0 CC(C)(C)OC(=O)N1CCC(Nc2ncnc3c(Nc4ccc(C#N)cc4F)ncnc23)CC1 10.1016/j.bmc.2018.06.035
56643412 79831 0 None -1 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 458 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010836 79831 0 None -1 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 458 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
60155365 84182 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 409 4 0 7 3.4 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(C#N)cc2)cn1 10.1021/jm300310c
CHEMBL2086670 84182 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 409 4 0 7 3.4 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(C#N)cc2)cn1 10.1021/jm300310c
89995541 153889 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 520 5 0 5 6.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cnc(-c4ccccc4)c3)c(Cl)c2)C2CC2)CC1 nan
CHEMBL3927436 153889 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 520 5 0 5 6.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cnc(-c4ccccc4)c3)c(Cl)c2)C2CC2)CC1 nan
67463144 153428 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 425 6 1 5 5.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccccc4)c3)oc2c1 nan
CHEMBL3923612 153428 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 425 6 1 5 5.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccccc4)c3)oc2c1 nan
62706851 83079 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 7 1 8 2.9 COC(=O)c1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058668 83079 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 7 1 8 2.9 COC(=O)c1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
89995519 152158 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1ncc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)o1 nan
CHEMBL3913786 152158 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1ncc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)o1 nan
71720494 93755 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 477 7 0 7 4.5 CC(C)(F)c1noc(N2CCC(COC3CC=C(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)n1 10.1021/ml300399u
CHEMBL2323595 93755 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 477 7 0 7 4.5 CC(C)(F)c1noc(N2CCC(COC3CC=C(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)n1 10.1021/ml300399u
11190983 68605 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 4 0 9 3.3 Cc1nn(-c2ccc(S(C)(=O)=O)cc2)c2ncnc(OC3CCN(C(=O)OC(C)(C)C)CC3)c12 10.1016/j.bmcl.2011.03.007
CHEMBL1773288 68605 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 4 0 9 3.3 Cc1nn(-c2ccc(S(C)(=O)=O)cc2)c2ncnc(OC3CCN(C(=O)OC(C)(C)C)CC3)c12 10.1016/j.bmcl.2011.03.007
127050520 147755 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 507 7 2 8 3.3 CCc1cnc(N2CCC(n3ncc4cc(-c5cc(F)c(C(=O)NCCO)cc5F)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
CHEMBL3823329 147755 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 507 7 2 8 3.3 CCc1cnc(N2CCC(n3ncc4cc(-c5cc(F)c(C(=O)NCCO)cc5F)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
137656911 166431 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 474 6 1 8 3.6 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(F)c1 10.1016/j.bmc.2017.06.014
CHEMBL4103709 166431 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 474 6 1 8 3.6 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(F)c1 10.1016/j.bmc.2017.06.014
72945518 111400 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 483 6 1 6 4.4 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C1CC1)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104889 111400 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 483 6 1 6 4.4 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C1CC1)C2=O 10.1016/j.bmcl.2013.11.053
46939910 169839 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(F)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4176348 169839 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(F)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
155528031 178043 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 457 4 0 7 4.1 CC1(C)C[C@]2(CC[C@H](Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)CO1 10.1016/j.bmcl.2018.12.041
CHEMBL4460354 178043 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 457 4 0 7 4.1 CC1(C)C[C@]2(CC[C@H](Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)CO1 10.1016/j.bmcl.2018.12.041
16036825 68007 0 None 7 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1766081 68007 0 None 7 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.04.035
76320655 110010 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 7 0 7 3.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084377 110010 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 7 0 7 3.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(C)C)c1C 10.1016/j.bmcl.2011.04.035
76313416 110021 0 None 14 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(C#N)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084388 110021 0 None 14 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(C#N)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
118722575 122935 0 None 14 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 463 5 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2F)cn1 10.1021/jm5011012
CHEMBL3357999 122935 0 None 14 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 463 5 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2F)cn1 10.1021/jm5011012
118720426 122683 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 501 5 2 8 3.2 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)nc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354799 122683 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 501 5 2 8 3.2 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)nc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354802 122683 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 501 5 2 8 3.2 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)nc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
71116111 130511 0 None -3 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 429 7 0 7 3.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)CC1 10.1021/acsmedchemlett.5b00207
CHEMBL3622169 130511 0 None -3 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 429 7 0 7 3.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)CC1 10.1021/acsmedchemlett.5b00207
118720416 122672 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.5 COC(=O)C1(Cc2ccccc2)COc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354788 122672 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.5 COC(=O)C1(Cc2ccccc2)COc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
89995523 151600 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 441 5 0 6 4.0 COC1CN(C(=O)OC(C)(C)C)CCC1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
CHEMBL3909522 151600 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 441 5 0 6 4.0 COC1CN(C(=O)OC(C)(C)C)CCC1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
73388221 156797 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.6 CC1CN(C(=O)OC(C)(C)C)CCC1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
CHEMBL3950359 156797 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.6 CC1CN(C(=O)OC(C)(C)C)CCC1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
21897897 68601 0 None -2 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 489 4 0 9 3.7 CC(C)(C)OC(=O)N1CCC(Sc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773282 68601 0 None -2 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 489 4 0 9 3.7 CC(C)(C)OC(=O)N1CCC(Sc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
51030900 116196 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
CHEMBL3220033 116196 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
51030899 116197 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
CHEMBL3220034 116197 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
90666910 116231 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 492 5 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220236 116231 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 492 5 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
118722574 122934 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 512 7 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2)cn1 10.1021/jm5011012
CHEMBL3357998 122934 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 512 7 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2)cn1 10.1021/jm5011012
76324930 111697 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 557 6 0 6 7.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)cs4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112989 111697 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 557 6 0 6 7.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)cs4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
67450901 129076 0 None -3 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 469 6 0 9 2.0 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC4CCOC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598102 129076 0 None -3 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 469 6 0 9 2.0 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC4CCOC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
118711787 120814 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 5 0 8 2.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326679 120814 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 5 0 8 2.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
89995652 158758 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 424 4 0 5 4.1 Cn1cncc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3966709 158758 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 424 4 0 5 4.1 Cn1cncc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
118711217 120712 0 None -7 2 Rat 5.8 pEC50 = 5.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325850 120712 0 None -7 2 Rat 5.8 pEC50 = 5.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
54591958 154053 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 420 6 1 6 3.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)N(C)C)cc3)oc2c1 nan
CHEMBL3928761 154053 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 420 6 1 6 3.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)N(C)C)cc3)oc2c1 nan
67463366 151492 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 1 4 3.1 O=C1NN=C(c2ccc3nc(-c4ccc(F)cc4)oc3c2)C2CC12 nan
CHEMBL3908693 151492 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 1 4 3.1 O=C1NN=C(c2ccc3nc(-c4ccc(F)cc4)oc3c2)C2CC12 nan
54591795 157466 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.3 Cc1ccc(-c2nc3ccc(C4=NNC(=O)C5CC45)cc3o2)cc1 nan
CHEMBL3955879 157466 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.3 Cc1ccc(-c2nc3ccc(C4=NNC(=O)C5CC45)cc3o2)cc1 nan
56960234 189487 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 532 7 1 9 4.8 O=C1NC(=O)/C(=C/c2cccc(Oc3cc(OC4CCN(C(=O)OCc5ccccc5)CC4)ncn3)c2)S1 10.1016/j.bmc.2021.116071
CHEMBL4789532 189487 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 532 7 1 9 4.8 O=C1NC(=O)/C(=C/c2cccc(Oc3cc(OC4CCN(C(=O)OCc5ccccc5)CC4)ncn3)c2)S1 10.1016/j.bmc.2021.116071
145969583 171967 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 451 7 0 5 5.1 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4228647 171967 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 451 7 0 5 5.1 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
60155459 84192 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 407 4 0 7 2.8 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3c(F)cncc3F)cn2)CC1 10.1021/jm300310c
CHEMBL2086682 84192 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 407 4 0 7 2.8 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3c(F)cncc3F)cn2)CC1 10.1021/jm300310c
137638009 162744 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 441 7 0 6 4.0 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)cc1 10.1016/j.bmcl.2017.06.032
CHEMBL4061409 162744 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 441 7 0 6 4.0 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)cc1 10.1016/j.bmcl.2017.06.032
71545537 93031 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.4 CC[C@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
CHEMBL2312527 93031 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.4 CC[C@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
67461016 154476 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 2 1 5 3.4 CC1CC(c2ccc3nc(-c4cccs4)oc3c2)=NNC1=O nan
CHEMBL3931941 154476 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 2 1 5 3.4 CC1CC(c2ccc3nc(-c4cccs4)oc3c2)=NNC1=O nan
67462822 152176 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCCCC4)c3)oc2c1 nan
CHEMBL3913957 152176 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCCCC4)c3)oc2c1 nan
137657254 166544 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 497 6 0 8 4.4 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)C)CC4)ncnc23)cc1 10.1016/j.bmcl.2017.06.032
CHEMBL4105139 166544 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 497 6 0 8 4.4 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)C)CC4)ncnc23)cc1 10.1016/j.bmcl.2017.06.032
60155273 84179 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1CN2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086667 84179 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1CN2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
54591336 151529 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 405 5 1 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOC4)cc3)oc2c1 nan
CHEMBL3908988 151529 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 405 5 1 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOC4)cc3)oc2c1 nan
145970536 171621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 501 5 1 7 4.4 CC(C)(C)OC(=O)N1CCC(c2nc(COc3ccc(/C=C4\CC(=O)NC4=O)cc3F)cs2)CC1 10.1016/j.bmcl.2017.10.046
CHEMBL4218908 171621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 501 5 1 7 4.4 CC(C)(C)OC(=O)N1CCC(c2nc(COc3ccc(/C=C4\CC(=O)NC4=O)cc3F)cs2)CC1 10.1016/j.bmcl.2017.10.046
89995704 152855 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 CC1CC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CCN1C(=O)OC(C)(C)C nan
CHEMBL3919153 152855 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 CC1CC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CCN1C(=O)OC(C)(C)C nan
67466181 153932 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 1 4 3.1 O=C1NN=C(c2ccc3nc(-c4ccccc4F)oc3c2)C2CC12 nan
CHEMBL3927783 153932 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 1 4 3.1 O=C1NN=C(c2ccc3nc(-c4ccccc4F)oc3c2)C2CC12 nan
56960792 186504 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 484 6 1 9 3.9 CCOC(=O)N1CCC(Oc2ncnc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)c2C)CC1 10.1016/j.bmc.2021.116071
CHEMBL4744049 186504 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 484 6 1 9 3.9 CCOC(=O)N1CCC(Oc2ncnc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)c2C)CC1 10.1016/j.bmc.2021.116071
89995558 155610 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 369 4 0 5 3.2 COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3941058 155610 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 369 4 0 5 3.2 COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
118722580 122941 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 7 1 10 3.5 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=N)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358004 122941 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 7 1 10 3.5 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=N)=O)cc2F)cn1 10.1021/jm5011012
60155543 84236 0 None -6 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2nc(C3CC3)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2087085 84236 0 None -6 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2nc(C3CC3)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
62707006 83085 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 6 4.4 CC(C)c1noc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1016/j.bmcl.2012.05.117
CHEMBL2058674 83085 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 6 4.4 CC(C)c1noc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1016/j.bmcl.2012.05.117
89995543 160227 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 422 4 0 5 4.1 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cncnc3)cc2)C2CC2)CC1 nan
CHEMBL3979369 160227 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 422 4 0 5 4.1 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cncnc3)cc2)C2CC2)CC1 nan
67464489 153883 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 431 6 1 6 5.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cccs4)cc3)oc2c1 nan
CHEMBL3927383 153883 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 431 6 1 6 5.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cccs4)cc3)oc2c1 nan
58017000 89311 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 472 4 0 6 4.6 CC(C)(C)OC(=O)N1CCC(Oc2cccc3c2CCN3c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
CHEMBL2177779 89311 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 472 4 0 6 4.6 CC(C)(C)OC(=O)N1CCC(Oc2cccc3c2CCN3c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
58017038 89316 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 479 5 0 7 4.7 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(-c3cccn3C)cc2F)CC1 10.1021/jm301404a
CHEMBL2177784 89316 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 479 5 0 7 4.7 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(-c3cccn3C)cc2F)CC1 10.1021/jm301404a
71450290 89832 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 478 5 0 8 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)c(F)c2)CC1 10.1021/jm301404a
CHEMBL2181687 89832 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 478 5 0 8 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)c(F)c2)CC1 10.1021/jm301404a
90665950 116008 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nnc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)o1 10.1039/C2MD20130E
CHEMBL3217767 116008 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nnc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)o1 10.1039/C2MD20130E
51030900 116196 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
CHEMBL3220033 116196 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
51030899 116197 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
CHEMBL3220034 116197 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 7 0 11 2.1 CO[C@@H](C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
90666910 116231 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 492 5 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220236 116231 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 492 5 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
58190317 116232 0 None -7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 478 5 0 9 2.3 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220237 116232 0 None -7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 478 5 0 9 2.3 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
89995712 150812 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 410 5 0 5 3.8 Cc1nccn1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)C)CC2)cc1 nan
CHEMBL3903019 150812 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 410 5 0 5 3.8 Cc1nccn1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)C)CC2)cc1 nan
24899747 89297 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 484 6 0 8 1.9 CCS(=O)(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177764 89297 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 484 6 0 8 1.9 CCS(=O)(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
90666916 116239 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 410 5 0 9 1.4 C[C@@H]1CN(C(=O)OC2COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220244 116239 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 410 5 0 9 1.4 C[C@@H]1CN(C(=O)OC2COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
54590842 153905 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 427 6 1 7 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cncnc4)cc3)oc2c1 nan
CHEMBL3927551 153905 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 427 6 1 7 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cncnc4)cc3)oc2c1 nan
62706849 83077 0 None -1 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 380 7 1 6 3.7 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058666 83077 0 None -1 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 380 7 1 6 3.7 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
67464592 159758 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 464 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC(F)CC4)cc3)oc2c1 nan
CHEMBL3975234 159758 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 464 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC(F)CC4)cc3)oc2c1 nan
66556121 93750 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 451 5 0 5 4.8 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1021/ml300399u
CHEMBL2323590 93750 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 451 5 0 5 4.8 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1021/ml300399u
162663470 188732 0 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4779950 188732 0 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116208
71655179 97523 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 466 7 1 6 5.2 CCOC(=O)c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391593 97523 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 466 7 1 6 5.2 CCOC(=O)c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
72946092 111391 0 None 4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104879 111391 0 None 4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
68040003 130770 0 None 8 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 484 5 0 8 4.1 Cc1c(Oc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629477 130770 0 None 8 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 484 5 0 8 4.1 Cc1c(Oc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
155553659 180905 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 470 4 0 7 4.1 CN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4545952 180905 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 470 4 0 7 4.1 CN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
54589269 117671 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 562 9 1 7 3.7 CCCc1cnc(N2CCC(C3Cc4c(F)c(C5=CCN(S(=O)(=O)CCCO)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261140 117671 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 562 9 1 7 3.7 CCCc1cnc(N2CCC(C3Cc4c(F)c(C5=CCN(S(=O)(=O)CCCO)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
71546036 93010 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 451 4 0 7 4.7 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312506 93010 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 451 4 0 7 4.7 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
66964622 117520 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 405 6 0 5 4.9 CCOC(=O)C(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260512 117520 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 405 6 0 5 4.9 CCOC(=O)C(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
60155366 84185 0 None 8 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 487 5 0 9 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm300310c
CHEMBL2086673 84185 0 None 8 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 487 5 0 9 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm300310c
58074082 111857 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 497 3 0 8 4.1 CC(C)(C)OC(=O)N1CCC(n2ccc3c(N4CCc5cc(S(C)(=O)=O)ccc54)ncnc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113843 111857 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 497 3 0 8 4.1 CC(C)(C)OC(=O)N1CCC(n2ccc3c(N4CCc5cc(S(C)(=O)=O)ccc54)ncnc32)CC1 10.1016/j.bmc.2014.01.028
137643239 165079 0 None 4 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 414 8 1 5 3.5 NC(=O)Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1 10.1016/j.bmcl.2017.01.091
CHEMBL4089040 165079 0 None 4 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 414 8 1 5 3.5 NC(=O)Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1 10.1016/j.bmcl.2017.01.091
53492467 129054 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598081 129054 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
25053111 195788 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 499 8 1 11 3.3 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(CC5CC5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL508869 195788 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 499 8 1 11 3.3 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(CC5CC5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
71655180 97524 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 432 7 1 6 4.5 CCOC(=O)c1ccnc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391594 97524 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 432 7 1 6 4.5 CCOC(=O)c1ccnc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
76335868 111805 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 3.8 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)c(F)cc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113634 111805 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 3.8 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)c(F)cc32)CC1 10.1016/j.bmc.2014.01.028
118722586 122950 0 None -8 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 504 8 0 10 3.0 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(CS(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
CHEMBL3358013 122950 0 None -8 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 504 8 0 10 3.0 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(CS(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
71655013 97539 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 424 6 1 7 4.1 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc([N+](=O)[O-])cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391609 97539 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 424 6 1 7 4.1 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc([N+](=O)[O-])cc3)c2)n1 10.1016/j.bmcl.2013.04.014
46884938 14811 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 466 9 0 6 2.6 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)CC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1090880 14811 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 466 9 0 6 2.6 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)CC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
122194421 130793 0 None -5 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 3.2 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2015.09.047
CHEMBL3629598 130793 0 None -5 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 3.2 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2015.09.047
60155184 84170 0 None -1 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086658 84170 0 None -1 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
67462896 154772 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 334 3 2 5 2.8 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(CN)c3)oc2c1 nan
CHEMBL3934223 154772 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 334 3 2 5 2.8 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(CN)c3)oc2c1 nan
162663967 188941 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level incubated for 45 mins by cAMP HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level incubated for 45 mins by cAMP HTRF assay
ChEMBL 408 4 0 8 2.4 CC(C)(C)OC(=O)N1CC2(C1)CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1021/acsmedchemlett.9b00248
CHEMBL4782474 188941 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level incubated for 45 mins by cAMP HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level incubated for 45 mins by cAMP HTRF assay
ChEMBL 408 4 0 8 2.4 CC(C)(C)OC(=O)N1CC2(C1)CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1021/acsmedchemlett.9b00248
62706853 83081 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1nc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)no1 10.1016/j.bmcl.2012.05.117
CHEMBL2058670 83081 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1nc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)no1 10.1016/j.bmcl.2012.05.117
60155183 84169 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 449 5 0 9 1.9 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
CHEMBL2086657 84169 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 449 5 0 9 1.9 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
118300928 158382 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 555 6 1 5 5.4 CC(C)(C)NS(=O)(=O)c1ccccc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3963502 158382 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 555 6 1 5 5.4 CC(C)(C)NS(=O)(=O)c1ccccc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
67466150 167060 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@@H]2CCc3nc(-c4ccccc4)oc3C2)[C@@H]2C[C@H]12 nan
CHEMBL4110302 167060 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@@H]2CCc3nc(-c4ccccc4)oc3C2)[C@@H]2C[C@H]12 nan
53492397 129082 0 None -2 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 477 7 0 7 3.4 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598108 129082 0 None -2 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 477 7 0 7 3.4 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
71546034 93008 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.3 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312504 93008 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.3 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
66964195 117542 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 462 5 0 5 6.3 Cc1cnc(C(C)(Cc2ccccc2)c2ccnc3c(-c4ccc(C(F)(F)F)cc4)cnn23)o1 10.1016/j.bmcl.2014.03.023
CHEMBL3260538 117542 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 462 5 0 5 6.3 Cc1cnc(C(C)(Cc2ccccc2)c2ccnc3c(-c4ccc(C(F)(F)F)cc4)cnn23)o1 10.1016/j.bmcl.2014.03.023
67462528 167549 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 6 2 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@H]4CCCN4)cc3)oc2c1 nan
CHEMBL4114154 167549 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 6 2 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@H]4CCCN4)cc3)oc2c1 nan
54584841 68346 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 387 3 1 4 3.6 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(C(N)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771073 68346 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 387 3 1 4 3.6 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(C(N)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
76320656 110014 0 None 3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 510 7 1 8 2.9 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084381 110014 0 None 3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 510 7 1 8 2.9 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
54591872 154618 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 2 1 4 3.6 C[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3933014 154618 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 2 1 4 3.6 C[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
118711783 120810 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326675 120810 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
62706030 83084 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 378 7 1 5 4.3 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058673 83084 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 378 7 1 5 4.3 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)nc1 10.1016/j.bmcl.2012.05.117
68229751 129057 0 None -3 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)c(F)c3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598084 129057 0 None -3 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)c(F)c3)CC2)CC1 10.1016/j.bmcl.2015.04.102
118711212 120707 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325845 120707 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711218 120713 0 None -8 2 Rat 5.8 pEC50 = 5.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325851 120713 0 None -8 2 Rat 5.8 pEC50 = 5.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
140254101 173378 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 574 6 0 6 5.7 O=C(OCC(F)(F)F)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4280383 173378 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 574 6 0 6 5.7 O=C(OCC(F)(F)F)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
71545700 93022 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 516 5 0 8 4.0 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312519 93022 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 516 5 0 8 4.0 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
66574514 120801 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2015.04.102
CHEMBL3326667 120801 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2015.04.102
73388331 155177 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 1 6 3.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)c(N)c2)C2CC2)CC1 nan
CHEMBL3937555 155177 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 1 6 3.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)c(N)c2)C2CC2)CC1 nan
66574514 120801 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326667 120801 0 None -12 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 480 6 0 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
25053184 183478 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 501 8 1 11 3.8 CCS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL459873 183478 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 501 8 1 11 3.8 CCS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
25260830 111854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116208
CHEMBL3113840 111854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116208
140253898 173604 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 642 6 0 6 6.7 O=C(OC(C(F)(F)F)C(F)(F)F)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4284899 173604 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 642 6 0 6 6.7 O=C(OC(C(F)(F)F)C(F)(F)F)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
122194337 130771 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
CHEMBL3629478 130771 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
88567661 169173 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 463 5 1 8 3.4 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3cccnc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4165734 169173 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 463 5 1 8 3.4 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3cccnc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
71546857 92957 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 490 4 0 10 3.7 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312156 92957 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 490 4 0 10 3.7 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
70796891 117525 0 None 11 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260518 117525 0 None 11 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
25260830 111854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113840 111854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2014.01.028
118720407 122663 0 None -8 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 451 4 0 5 5.0 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354779 122663 0 None -8 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 451 4 0 5 5.0 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
11397354 7839 2 None -23 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5741 7839 2 None -23 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1773293 7839 2 None -23 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
25053187 183699 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 485 8 1 10 4.1 CC[S+]([O-])c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL461933 183699 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 485 8 1 10 4.1 CC[S+]([O-])c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
118711790 120816 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 488 7 0 8 2.9 CCC(F)(F)C(=O)N1CCC(Oc2ncnc(Oc3ccc(S(C)(=O)=O)nc3C)c2F)CC1 10.1016/j.bmcl.2014.06.071
CHEMBL3326681 120816 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 488 7 0 8 2.9 CCC(F)(F)C(=O)N1CCC(Oc2ncnc(Oc3ccc(S(C)(=O)=O)nc3C)c2F)CC1 10.1016/j.bmcl.2014.06.071
66964044 117530 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 385 6 0 5 4.9 CCOC(=O)C(C)(CC(C)C)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260524 117530 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 385 6 0 5 4.9 CCOC(=O)C(C)(CC(C)C)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
54592033 156614 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 445 7 1 5 6.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCC4CCCCC4)cc3)oc2c1 nan
CHEMBL3948883 156614 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 445 7 1 5 6.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCC4CCCCC4)cc3)oc2c1 nan
10094886 180181 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 442 9 0 9 3.5 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(CCC(C)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL452824 180181 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 442 9 0 9 3.5 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(CCC(C)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
145982637 172453 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 490 4 2 9 4.5 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc3c(Nc4ccc(C#N)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4244903 172453 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 490 4 2 9 4.5 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc3c(Nc4ccc(C#N)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
76324996 111849 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 482 5 0 7 3.6 COc1cc(S(C)(=O)=O)cc2c1N(C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1)CC2 10.1016/j.bmc.2014.01.028
CHEMBL3113836 111849 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 482 5 0 7 3.6 COc1cc(S(C)(=O)=O)cc2c1N(C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1)CC2 10.1016/j.bmc.2014.01.028
54591720 151315 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.3 Cc1c(C2=NNC(=O)C3CC23)ccc2nc(-c3ccccc3)oc12 nan
CHEMBL3907256 151315 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.3 Cc1c(C2=NNC(=O)C3CC23)ccc2nc(-c3ccccc3)oc12 nan
137632997 163162 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 455 6 0 6 4.4 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)(C)C)CC3)cn2)cc1 10.1016/j.bmcl.2017.06.032
CHEMBL4066367 163162 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 455 6 0 6 4.4 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)(C)C)CC3)cn2)cc1 10.1016/j.bmcl.2017.06.032
89995702 157403 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 478 5 1 5 4.1 CNC(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)nc1 nan
CHEMBL3955383 157403 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 478 5 1 5 4.1 CNC(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)nc1 nan
71655016 97542 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 399 5 1 5 4.5 Cc1ccc(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391612 97542 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 399 5 1 5 4.5 Cc1ccc(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
70685175 79841 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 488 7 0 7 3.0 CO[C@H]1CN(Cc2ccc(C(F)(F)F)cc2)CC[C@H]1N(C)C(=O)Cc1ccc(-n2cnnn2)cc1 10.1016/j.bmcl.2011.10.033
CHEMBL2010847 79841 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 488 7 0 7 3.0 CO[C@H]1CN(Cc2ccc(C(F)(F)F)cc2)CC[C@H]1N(C)C(=O)Cc1ccc(-n2cnnn2)cc1 10.1016/j.bmcl.2011.10.033
118709765 120330 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 470 5 0 7 3.6 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3)csc12)C1CCN(C(=O)C2CC2)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321831 120330 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 470 5 0 7 3.6 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3)csc12)C1CCN(C(=O)C2CC2)CC1 10.1016/j.bmcl.2014.07.020
67465164 166983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 353 4 1 5 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccsc4)oc3c2)[C@@H]1C nan
CHEMBL4109572 166983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 353 4 1 5 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccsc4)oc3c2)[C@@H]1C nan
89995650 158387 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@@H](F)C1 nan
CHEMBL3963533 158387 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@@H](F)C1 nan
90000794 153796 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 477 6 0 4 5.4 CN(C)Cc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
CHEMBL3926629 153796 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 477 6 0 4 5.4 CN(C)Cc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
57390603 77605 0 None -6 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 397 5 0 8 3.2 Cc1c(Oc2cncc(C#N)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951019 77605 0 None -6 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 397 5 0 8 3.2 Cc1c(Oc2cncc(C#N)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
54591868 160261 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 402 4 1 6 2.8 O=C1NN=C(c2ccc3nc(-c4ccc(CN5CCOCC5)cc4)oc3c2)C2CC12 nan
CHEMBL3979605 160261 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 402 4 1 6 2.8 O=C1NN=C(c2ccc3nc(-c4ccc(CN5CCOCC5)cc4)oc3c2)C2CC12 nan
76335131 109997 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 426 4 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084363 109997 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 426 4 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
118711794 120820 0 None -8 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 520 7 0 11 2.7 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)C)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326685 120820 0 None -8 2 Rat 6.8 pEC50 = 6.8 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 520 7 0 11 2.7 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)C)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
73387915 150719 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 497 6 0 6 3.9 CC1(OC(=O)N2CCC(N(C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)C3CC3)CC2)CC1 nan
CHEMBL3902324 150719 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 497 6 0 6 3.9 CC1(OC(=O)N2CCC(N(C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)C3CC3)CC2)CC1 nan
127048479 147698 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 458 5 0 8 3.8 CC(C)OC(=O)N1CCC(n2ncc3cc(Oc4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3822545 147698 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 458 5 0 8 3.8 CC(C)OC(=O)N1CCC(n2ncc3cc(Oc4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
118300926 157928 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 498 5 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3)cc2)C2CC2)CC1 nan
CHEMBL3959546 157928 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 498 5 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3)cc2)C2CC2)CC1 nan
145985013 172397 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 525 5 2 10 3.8 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1C[C@@H]2Nc1ncnc2c(Nc3ccc(S(C)(=O)=O)cc3)ncnc12 10.1016/j.bmc.2018.06.035
CHEMBL4243251 172397 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 525 5 2 10 3.8 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1C[C@@H]2Nc1ncnc2c(Nc3ccc(S(C)(=O)=O)cc3)ncnc12 10.1016/j.bmc.2018.06.035
86694585 140971 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 513 4 0 8 4.1 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(c5nnc(C(F)(F)F)s5)CC4)oc3cn2)CC1 nan
CHEMBL3716724 140971 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 513 4 0 8 4.1 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(c5nnc(C(F)(F)F)s5)CC4)oc3cn2)CC1 nan
54585808 68361 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 413 4 0 5 3.9 Cc1ccc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771090 68361 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 413 4 0 5 3.9 Cc1ccc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
54581962 68370 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771099 68370 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
164627746 193285 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 515 6 0 8 4.2 CCCN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
CHEMBL4877468 193285 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 515 6 0 8 4.2 CCCN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
145967361 170962 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 503 7 1 8 4.2 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)NC5=O)cc4C)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4210640 170962 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 503 7 1 8 4.2 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)NC5=O)cc4C)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
140251528 171718 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 441 7 0 5 4.4 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4224814 171718 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 441 7 0 5 4.4 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
137637929 163045 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 490 6 1 8 4.1 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1Cl 10.1016/j.bmc.2017.06.014
CHEMBL4065009 163045 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 490 6 1 8 4.1 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1Cl 10.1016/j.bmc.2017.06.014
137659062 166068 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 470 6 1 8 3.7 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1C 10.1016/j.bmc.2017.06.014
CHEMBL4099540 166068 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 470 6 1 8 3.7 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1C 10.1016/j.bmc.2017.06.014
76335131 109997 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 426 4 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084363 109997 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 426 4 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
76309728 109999 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 5 0 7 4.3 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC2(C)CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084365 109999 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 5 0 7 4.3 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC2(C)CC2)c1C 10.1016/j.bmcl.2011.04.035
76320659 110023 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 410 5 0 7 4.0 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084390 110023 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 410 5 0 7 4.0 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
118722586 122950 0 None 8 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 504 8 0 10 3.0 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(CS(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
CHEMBL3358013 122950 0 None 8 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 504 8 0 10 3.0 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(CS(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
70687332 79848 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 493 6 0 6 3.5 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)[C@@H]1CCN(Cc2nc3cc(F)ccc3s2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010853 79848 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 493 6 0 6 3.5 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)[C@@H]1CCN(Cc2nc3cc(F)ccc3s2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
54581962 68370 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771099 68370 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
53491781 129064 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 483 6 0 8 3.8 CC(C)S(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598091 129064 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 483 6 0 8 3.8 CC(C)S(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
76328493 111688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 516 5 0 7 5.7 Cc1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
CHEMBL3112980 111688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 516 5 0 7 5.7 Cc1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
76321325 111718 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 586 7 0 9 5.0 CS(=O)(=O)c1cccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)c1 10.1016/j.bmcl.2013.12.127
CHEMBL3113010 111718 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 586 7 0 9 5.0 CS(=O)(=O)c1cccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)c1 10.1016/j.bmcl.2013.12.127
66964068 117535 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccccc3Cl)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260529 117535 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccccc3Cl)cnn12 10.1016/j.bmcl.2014.03.023
76331521 110019 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 439 6 1 7 3.3 Cc1c(Nc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084386 110019 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 439 6 1 7 3.3 Cc1c(Nc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
46884904 14849 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 508 7 0 8 3.3 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)c4cccs4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1091203 14849 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 508 7 0 8 3.3 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)c4cccs4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
71717334 93114 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 438 6 1 7 3.2 CC(C)OC(=O)N1CCC(n2cc(CNc3ccc(S(C)(=O)=O)cc3F)cn2)CC1 10.1016/j.bmcl.2012.10.119
CHEMBL2313405 93114 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 438 6 1 7 3.2 CC(C)OC(=O)N1CCC(n2cc(CNc3ccc(S(C)(=O)=O)cc3F)cn2)CC1 10.1016/j.bmcl.2012.10.119
54591569 151865 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 488 9 1 6 5.6 CCCC1CCN(CCOc2ccc(-c3nc4ccc(C5=NNC(=O)CC5CC)cc4o3)cc2)CC1 nan
CHEMBL3911614 151865 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 488 9 1 6 5.6 CCCC1CCN(CCOc2ccc(-c3nc4ccc(C5=NNC(=O)CC5CC)cc4o3)cc2)CC1 nan
67462510 159931 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 3 1 4 3.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3976697 159931 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 3 1 4 3.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
67466188 159716 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 5 2 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCNCC4)cc3)oc2c1 nan
CHEMBL3974996 159716 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 5 2 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCNCC4)cc3)oc2c1 nan
145965514 171038 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 489 7 1 8 3.9 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)NC5=O)cc4)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4211568 171038 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 489 7 1 8 3.9 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)NC5=O)cc4)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
145971166 171920 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 423 5 0 5 4.3 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4227878 171920 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 423 5 0 5 4.3 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
60155460 84193 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 399 4 0 7 3.2 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)C[C@H]2C)nc1 10.1021/jm300310c
CHEMBL2086683 84193 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 399 4 0 7 3.2 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)C[C@H]2C)nc1 10.1021/jm300310c
162643194 188459 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 562 9 1 12 0.8 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(CCC)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4776485 188459 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 562 9 1 12 0.8 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(CCC)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
60155099 84167 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086654 84167 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
67464757 150083 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4C(C)C)cc3)oc2c1 nan
CHEMBL3897121 150083 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4C(C)C)cc3)oc2c1 nan
118711218 120713 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325851 120713 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
56960372 188621 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 456 5 1 9 3.2 COC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4778466 188621 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 456 5 1 9 3.2 COC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
68036822 169881 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 517 6 1 9 3.4 CC1(COC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)COC1 10.1021/acsmedchemlett.8b00073
CHEMBL4177077 169881 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 517 6 1 9 3.4 CC1(COC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)COC1 10.1021/acsmedchemlett.8b00073
67462637 151615 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 CC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3909650 151615 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 CC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
67464711 158309 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 6 1 5 4.5 CCCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1 nan
CHEMBL3962903 158309 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 6 1 5 4.5 CCCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1 nan
70683089 79833 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 459 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010839 79833 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 459 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2011.10.033
54591023 152615 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 330 2 1 6 2.2 CC1CC(=O)NN=C1c1ccc2nc(N3CCSCC3)oc2c1 nan
CHEMBL3917177 152615 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 330 2 1 6 2.2 CC1CC(=O)NN=C1c1ccc2nc(N3CCSCC3)oc2c1 nan
86694579 141485 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 447 4 0 6 3.6 CC(C)OC(=O)N1CCC(c2cc3cc(C4=CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
CHEMBL3718464 141485 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 447 4 0 6 3.6 CC(C)OC(=O)N1CCC(c2cc3cc(C4=CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
54586779 68360 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 417 4 0 5 3.8 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771089 68360 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 417 4 0 5 3.8 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
54586780 68367 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C)nc(C#N)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
CHEMBL1771096 68367 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C)nc(C#N)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
145970276 170641 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 497 5 1 7 4.6 Cc1cc(/C=C2\CC(=O)NC2=O)ccc1OCc1csc(C2CCN(C(=O)OC(C)(C)C)CC2)n1 10.1016/j.bmcl.2017.10.046
CHEMBL4206682 170641 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 497 5 1 7 4.6 Cc1cc(/C=C2\CC(=O)NC2=O)ccc1OCc1csc(C2CCN(C(=O)OC(C)(C)C)CC2)n1 10.1016/j.bmcl.2017.10.046
137643188 164936 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 470 6 1 8 3.7 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(C)c1 10.1016/j.bmc.2017.06.014
CHEMBL4087339 164936 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 470 6 1 8 3.7 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(C)c1 10.1016/j.bmc.2017.06.014
72945517 111399 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 499 7 1 7 4.1 COc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C1CC1)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104888 111399 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 499 7 1 7 4.1 COc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C1CC1)C2=O 10.1016/j.bmcl.2013.11.053
72945711 111407 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 501 6 1 6 5.0 Cc1cc2c(c(Sc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104896 111407 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 501 6 1 6 5.0 Cc1cc2c(c(Sc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
68036951 169630 0 None 14 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 513 6 1 10 3.1 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(-n4cncn4)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4172962 169630 0 None 14 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 513 6 1 10 3.1 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(-n4cncn4)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
155568311 182856 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 448 5 2 7 4.3 CC1(C)C[C@]2(CC[C@H](Nc3cc(Nc4ccc(S(C)(=O)=O)cc4F)ncn3)CC2)CO1 10.1016/j.bmcl.2018.12.041
CHEMBL4591100 182856 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 448 5 2 7 4.3 CC1(C)C[C@]2(CC[C@H](Nc3cc(Nc4ccc(S(C)(=O)=O)cc4F)ncn3)CC2)CO1 10.1016/j.bmcl.2018.12.041
51029876 84172 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086660 84172 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
51030710 96978 0 None 70 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382416 96978 0 None 70 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
51029876 84172 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086660 84172 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
66964295 117538 0 None -7 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260533 117538 0 None -7 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
89995709 156327 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 444 5 0 5 4.4 CC1(OC(=O)N2CCC(N(C(=O)c3ccc(-c4ccncc4C#N)cc3)C3CC3)CC2)CC1 nan
CHEMBL3946672 156327 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 444 5 0 5 4.4 CC1(OC(=O)N2CCC(N(C(=O)c3ccc(-c4ccncc4C#N)cc3)C3CC3)CC2)CC1 nan
67606673 90450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 423 5 0 7 3.7 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)CC1 10.1021/ml300296q
CHEMBL2204986 90450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 423 5 0 7 3.7 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)CC1 10.1021/ml300296q
53630394 7873 0 None -21 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5738 7873 0 None -21 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1775178 7873 0 None -21 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
118711215 120710 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 500 7 0 9 3.2 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325848 120710 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 500 7 0 9 3.2 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
24897005 89317 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 4 0 8 3.5 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177785 89317 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 4 0 8 3.5 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
58190317 116232 0 None 7 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 478 5 0 9 2.3 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220237 116232 0 None 7 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 478 5 0 9 2.3 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
76310374 111691 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 584 6 0 7 6.5 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(CC(F)(F)F)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112983 111691 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 584 6 0 7 6.5 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(CC(F)(F)F)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
66963820 117523 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 371 6 0 5 4.3 CCOC(=O)C(Cc1ccccc1)c1ccnc2c(-c3ccccc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260515 117523 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 371 6 0 5 4.3 CCOC(=O)C(Cc1ccccc1)c1ccnc2c(-c3ccccc3)cnn12 10.1016/j.bmcl.2014.03.023
66963969 117526 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 447 8 0 5 5.9 CCCC(Cc1ccccc1)(C(=O)OCC)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260520 117526 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 447 8 0 5 5.9 CCCC(Cc1ccccc1)(C(=O)OCC)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
122194338 130772 0 None -4 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 538 5 1 9 4.1 Cc1c(Nc2ccc(S(C)(=O)=O)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
CHEMBL3629479 130772 0 None -4 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 538 5 1 9 4.1 Cc1c(Nc2ccc(S(C)(=O)=O)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
57399344 77607 0 None -7 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951021 77607 0 None -7 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
134132485 151885 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 499 5 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CC1CCN(C(=O)OC(C)C)CC1)c(=O)n2C 10.1016/j.ejmech.2016.08.023
CHEMBL3911786 151885 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 499 5 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CC1CCN(C(=O)OC(C)C)CC1)c(=O)n2C 10.1016/j.ejmech.2016.08.023
4993934 180182 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 450 7 0 10 2.4 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(S(C)(=O)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL452825 180182 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 450 7 0 10 2.4 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(S(C)(=O)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
54585806 68341 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 422 3 0 5 4.0 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cccc(S(C)(=O)=O)c3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771069 68341 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 422 3 0 5 4.0 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cccc(S(C)(=O)=O)c3)CC2)CC1 10.1016/j.bmcl.2010.12.086
46884820 15066 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 456 6 0 7 3.3 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(C(=O)c4ccco4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1092631 15066 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 456 6 0 7 3.3 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(C(=O)c4ccco4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
11462546 9997 43 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assayAgonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assay
ChEMBL 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 10.1021/acs.jmedchem.5b01198
3319 9997 43 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assayAgonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assay
ChEMBL 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 10.1021/acs.jmedchem.5b01198
CHEMBL1081913 9997 43 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assayAgonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assay
ChEMBL 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 10.1021/acs.jmedchem.5b01198
72946092 111391 0 None -120 4 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 assessed as cAMP accumulationAgonist activity at mouse GPR119 assessed as cAMP accumulation
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104879 111391 0 None -120 4 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 assessed as cAMP accumulationAgonist activity at mouse GPR119 assessed as cAMP accumulation
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
24958872 68339 0 None -5 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 2 0 3 4.9 Cc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771067 68339 0 None -5 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 2 0 3 4.9 Cc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
67467352 167717 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@H]4CCCN4C(C)C)cc3)oc2c1 nan
CHEMBL4115459 167717 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@H]4CCCN4C(C)C)cc3)oc2c1 nan
89995542 153383 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 502 6 0 6 5.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3noc(Cc4ccccc4)n3)cc2)C2CC2)CC1 nan
CHEMBL3923197 153383 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 502 6 0 6 5.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3noc(Cc4ccccc4)n3)cc2)C2CC2)CC1 nan
51029782 84189 1 None -26 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 401 5 0 8 2.5 COc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
CHEMBL2086678 84189 1 None -26 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 401 5 0 8 2.5 COc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
68209201 158728 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 411 5 1 5 4.9 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccccc4)c3)oc2c1 nan
CHEMBL3966469 158728 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 411 5 1 5 4.9 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccccc4)c3)oc2c1 nan
141750308 189984 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 602 8 1 13 1.6 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3nc(-c4ccccc4)ns3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4795875 189984 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 602 8 1 13 1.6 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3nc(-c4ccccc4)ns3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
54590934 152865 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 3 1 5 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C)s3)oc2c1 nan
CHEMBL3919254 152865 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 3 1 5 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C)s3)oc2c1 nan
118711217 120712 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325850 120712 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 486 7 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)CF)CC2)c1F 10.1016/j.bmcl.2014.06.071
67451300 129081 0 None -2 2 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 437 6 0 7 2.6 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598107 129081 0 None -2 2 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 437 6 0 7 2.6 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
54591186 156026 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 503 7 1 7 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccc(S(C)(=O)=O)cc4)cc3)oc2c1 nan
CHEMBL3944330 156026 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 503 7 1 7 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccc(S(C)(=O)=O)cc4)cc3)oc2c1 nan
127048481 147823 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 443 4 0 8 3.1 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)nc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3824150 147823 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 443 4 0 8 3.1 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)nc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
67465905 160497 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC(C)CC4)cc3)oc2c1 nan
CHEMBL3981612 160497 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC(C)CC4)cc3)oc2c1 nan
118722571 122931 0 None -36 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 523 6 0 11 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm5011012
CHEMBL3357995 122931 0 None -36 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 523 6 0 11 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm5011012
137637925 163043 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 504 7 0 9 4.4 CCc1cnc(N2CCC(Oc3ncnc4c(-c5ccc(C(=O)N(C)OC)cc5)csc34)CC2)nc1 10.1016/j.bmcl.2017.06.032
CHEMBL4064998 163043 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 504 7 0 9 4.4 CCc1cnc(N2CCC(Oc3ncnc4c(-c5ccc(C(=O)N(C)OC)cc5)csc34)CC2)nc1 10.1016/j.bmcl.2017.06.032
90666911 116233 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 452 6 0 9 2.4 CC(C)C1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
CHEMBL3220238 116233 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 452 6 0 9 2.4 CC(C)C1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
90666912 116234 0 None 5 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 438 6 0 9 2.1 CCC1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
CHEMBL3220239 116234 0 None 5 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 438 6 0 9 2.1 CCC1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
90666913 116235 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)OC2(C)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220240 116235 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)OC2(C)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
24898315 89303 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 474 4 1 9 1.9 CS(=O)(=O)c1ccc(N2CCc3c(OC4CCN(C5=NCCCN5)CC4)ncnc32)c(F)c1 10.1021/jm301404a
CHEMBL2177771 89303 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 474 4 1 9 1.9 CS(=O)(=O)c1ccc(N2CCc3c(OC4CCN(C5=NCCCN5)CC4)ncnc32)c(F)c1 10.1021/jm301404a
58017008 89824 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 477 5 1 8 3.1 CC(C)OC(=O)N1CCC(Nc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181676 89824 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 477 5 1 8 3.1 CC(C)OC(=O)N1CCC(Nc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
54586778 68354 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1nc(C#N)cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)n1 10.1016/j.bmcl.2010.12.086
CHEMBL1771082 68354 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1nc(C#N)cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)n1 10.1016/j.bmcl.2010.12.086
25012524 68364 0 None 5 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 397 3 0 7 3.2 Cc1cc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
CHEMBL1771093 68364 0 None 5 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 397 3 0 7 3.2 Cc1cc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
44467183 68372 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 425 7 0 8 3.4 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cn3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771102 68372 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 425 7 0 8 3.4 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cn3)CC2)nc1 10.1016/j.bmcl.2010.12.086
54586781 68373 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 378 6 0 7 3.1 Cc1cnc(N2CCC([C@H]3C[C@H]3CCOc3nc(C)cc(C#N)n3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771103 68373 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 378 6 0 7 3.1 Cc1cnc(N2CCC([C@H]3C[C@H]3CCOc3nc(C)cc(C#N)n3)CC2)nc1 10.1016/j.bmcl.2010.12.086
137651958 164263 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 492 6 1 8 3.7 CCNC(=O)c1cc(F)c(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
CHEMBL4079458 164263 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 492 6 1 8 3.7 CCNC(=O)c1cc(F)c(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
70856302 165891 0 None 3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 470 9 0 6 4.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)n1 10.1016/j.bmcl.2017.01.091
CHEMBL4097638 165891 0 None 3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 470 9 0 6 4.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)n1 10.1016/j.bmcl.2017.01.091
68211791 117667 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 546 8 0 6 4.8 CCCc1cnc(N2CCC(C3Cc4c(F)c(C5=CCN(S(=O)(=O)CCC)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261136 117667 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 546 8 0 6 4.8 CCCc1cnc(N2CCC(C3Cc4c(F)c(C5=CCN(S(=O)(=O)CCC)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
71455832 90439 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 471 5 0 7 2.8 CCc1cnc(N2CCC(C3Cc4cc(C5CCN(S(C)(=O)=O)CC5)ncc4O3)CC2)nc1 10.1021/ml300296q
CHEMBL2204975 90439 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 471 5 0 7 2.8 CCc1cnc(N2CCC(C3Cc4cc(C5CCN(S(C)(=O)=O)CC5)ncc4O3)CC2)nc1 10.1021/ml300296q
71208589 90443 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 526 4 0 6 3.9 CS(=O)(=O)N1CC=C(c2cc3c(cn2)O[C@@H](C2CCN(c4ncc(C(F)(F)F)cc4F)CC2)C3)CC1 10.1021/ml300296q
CHEMBL2204979 90443 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 526 4 0 6 3.9 CS(=O)(=O)N1CC=C(c2cc3c(cn2)O[C@@H](C2CCN(c4ncc(C(F)(F)F)cc4F)CC2)C3)CC1 10.1021/ml300296q
118720407 122663 0 None 8 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 451 4 0 5 5.0 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354779 122663 0 None 8 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 451 4 0 5 5.0 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
118720423 122679 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 527 7 1 6 4.2 COCCN(C)C(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354795 122679 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 527 7 1 6 4.2 COCCN(C)C(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
91824767 122682 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 500 5 2 7 3.8 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354798 122682 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 500 5 2 7 3.8 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354801 122682 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 500 5 2 7 3.8 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
118720431 122686 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 482 5 2 5 5.0 OCc1nn2c3c(cnc2c1-c1ccc(C(F)(F)F)cc1)CN[C@]3(Cc1cccc(F)c1)C1CC1 10.1016/j.bmcl.2014.10.010
CHEMBL3354804 122686 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 482 5 2 5 5.0 OCc1nn2c3c(cnc2c1-c1ccc(C(F)(F)F)cc1)CN[C@]3(Cc1cccc(F)c1)C1CC1 10.1016/j.bmcl.2014.10.010
51030901 84203 0 None 25 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2noc(C(F)(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086693 84203 0 None 25 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2noc(C(F)(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
24961800 68353 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
CHEMBL1771081 68353 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)nc(C#N)n1 10.1016/j.bmcl.2010.12.086
54586778 68354 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1nc(C#N)cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)n1 10.1016/j.bmcl.2010.12.086
CHEMBL1771082 68354 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 385 2 0 6 3.5 Cc1nc(C#N)cc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)n1 10.1016/j.bmcl.2010.12.086
54587813 68369 0 None 1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771098 68369 0 None 1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
54586781 68373 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 378 6 0 7 3.1 Cc1cnc(N2CCC([C@H]3C[C@H]3CCOc3nc(C)cc(C#N)n3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771103 68373 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 378 6 0 7 3.1 Cc1cnc(N2CCC([C@H]3C[C@H]3CCOc3nc(C)cc(C#N)n3)CC2)nc1 10.1016/j.bmcl.2010.12.086
73291736 167502 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@H](F)C1 nan
CHEMBL4113795 167502 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@H](F)C1 nan
71116039 130518 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622175 130518 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
145984093 172386 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 543 5 2 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4242974 172386 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 543 5 2 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
117684497 166037 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4099186 166037 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 472 8 0 5 4.4 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1)N1CCC1 10.1016/j.bmcl.2017.01.091
89584050 163573 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 8 0 5 5.1 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCCCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4070965 163573 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 500 8 0 5 5.1 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CCCCC1 10.1016/j.bmcl.2017.01.091
71474021 130507 0 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 483 9 1 7 3.1 O=S(=O)(CCO)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
CHEMBL3622165 130507 0 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 483 9 1 7 3.1 O=S(=O)(CCO)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
71128813 130514 0 None -1 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 463 9 0 7 3.5 CCOc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622171 130514 0 None -1 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 463 9 0 7 3.5 CCOc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
122191631 130516 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 437 7 0 6 3.2 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(F)cn3)CC2)cc1F 10.1021/acsmedchemlett.5b00207
CHEMBL3622173 130516 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 437 7 0 6 3.2 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(F)cn3)CC2)cc1F 10.1021/acsmedchemlett.5b00207
71140721 130517 0 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 447 8 0 6 3.7 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622174 130517 0 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 447 8 0 6 3.7 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
164625935 193141 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 541 4 0 8 4.3 CC(C)(C)OC(=O)N1CCC(N(c2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
CHEMBL4875358 193141 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 541 4 0 8 4.3 CC(C)(C)OC(=O)N1CCC(N(c2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
71135255 130508 0 None -1 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 430 8 0 7 2.9 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622166 130508 0 None -1 2 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 430 8 0 7 2.9 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
145973632 169877 0 None 8 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 473 6 1 7 5.1 CC(C)COC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
CHEMBL4177039 169877 0 None 8 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 473 6 1 7 5.1 CC(C)COC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
11705608 7224 65 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
12151 7224 65 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
CHEMBL1775179 7224 65 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
164617859 191566 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 533 7 0 10 2.8 CC(C)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4851479 191566 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 533 7 0 10 2.8 CC(C)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
67633261 90449 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 431 6 0 8 3.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)nc1 10.1021/ml300296q
CHEMBL2204985 90449 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 431 6 0 8 3.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)nc1 10.1021/ml300296q
58074090 192709 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 551 6 0 10 4.1 CC(C)c1noc(N2CCC(N(c3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4869157 192709 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 551 6 0 10 4.1 CC(C)c1noc(N2CCC(N(c3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
54583896 68368 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771097 68368 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
127048787 147711 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 456 3 0 7 4.1 CC(C)(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3822759 147711 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 456 3 0 7 4.1 CC(C)(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
127048787 147711 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 456 3 0 7 4.1 CC(C)(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmc.2017.06.014
CHEMBL3822759 147711 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 456 3 0 7 4.1 CC(C)(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmc.2017.06.014
71655179 97523 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 466 7 1 6 5.2 CCOC(=O)c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.12.127
CHEMBL2391593 97523 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 466 7 1 6 5.2 CCOC(=O)c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.12.127
71655315 97531 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 504 7 1 7 6.2 CC(C)c1noc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)n1 10.1016/j.bmcl.2013.12.127
CHEMBL2391601 97531 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 504 7 1 7 6.2 CC(C)c1noc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)n1 10.1016/j.bmcl.2013.12.127
68240419 130774 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629481 130774 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
58190330 122947 0 None 7 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 562 7 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358010 122947 0 None 7 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 562 7 0 9 2.7 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
118720415 122671 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 489 7 0 6 6.2 CCOC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(Oc5ccccc5)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354787 122671 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 489 7 0 6 6.2 CCOC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(Oc5ccccc5)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
118720430 122685 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 513 5 2 7 3.4 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(C(N)=O)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354803 122685 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 513 5 2 7 3.4 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(C(N)=O)nn3c21 10.1016/j.bmcl.2014.10.010
66963512 117524 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260517 117524 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
66963587 117544 0 None 4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 454 6 0 6 4.9 CCOC(=O)[C@](C)(Cc1ccccc1)c1cnnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260540 117544 0 None 4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 454 6 0 6 4.9 CCOC(=O)[C@](C)(Cc1ccccc1)c1cnnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
51030984 84197 0 None 26 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086687 84197 0 None 26 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
72188621 96973 0 None 19 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382411 96973 0 None 19 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
51030984 84197 0 None 26 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086687 84197 0 None 26 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
73353420 96977 0 None -5 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382415 96977 0 None -5 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
68230212 129072 0 None -1 3 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 by HTRF cAMP assayAgonist activity at mouse GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598099 129072 0 None -1 3 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 by HTRF cAMP assayAgonist activity at mouse GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
70810684 93763 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 519 7 0 7 4.6 CS(=O)(=O)c1ccc([C@H]2CC[C@H](OCC3CCN(Cc4nc(C(F)(F)F)no4)CC3)CC2)c(F)c1 10.1021/ml300399u
CHEMBL2323603 93763 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 519 7 0 7 4.6 CS(=O)(=O)c1ccc([C@H]2CC[C@H](OCC3CCN(Cc4nc(C(F)(F)F)no4)CC3)CC2)c(F)c1 10.1021/ml300399u
4400062 117515 15 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 457 6 0 5 5.7 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260506 117515 15 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 457 6 0 5 5.7 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
46885171 14988 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 475 7 1 11 3.9 O=[N+]([O-])c1c(Nc2ccc(-n3cncn3)cc2)ncnc1N1CCC(Sc2ccccn2)CC1 10.1021/jm301404a
CHEMBL1092240 14988 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 475 7 1 11 3.9 O=[N+]([O-])c1c(Nc2ccc(-n3cncn3)cc2)ncnc1N1CCC(Sc2ccccn2)CC1 10.1021/jm301404a
46884902 14596 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 508 7 0 7 3.5 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)C4CCCCC4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1089528 14596 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 508 7 0 7 3.5 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)C4CCCCC4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
57399342 77599 0 None -5 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 466 6 1 8 3.5 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951012 77599 0 None -5 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 466 6 1 8 3.5 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
46885048 14634 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 476 8 0 7 2.5 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)c4ccco4)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1089837 14634 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 476 8 0 7 2.5 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)c4ccco4)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
46884903 14848 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 503 7 0 8 2.6 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)c4cccnc4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1091202 14848 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 503 7 0 8 2.6 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)c4cccnc4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
76324301 110018 0 None -37 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 429 6 1 7 3.1 Cc1ncccc1Nc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084385 110018 0 None -37 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 429 6 1 7 3.1 Cc1ncccc1Nc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
25012528 68356 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4cnccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771084 68356 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4cnccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
137648888 164120 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 494 4 0 9 3.6 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncc(F)cn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
CHEMBL4077670 164120 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 494 4 0 9 3.6 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncc(F)cn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
67449861 129060 0 None -15 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 440 6 0 7 3.2 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598087 129060 0 None -15 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 440 6 0 7 3.2 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
67464517 153282 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 3 1 4 2.9 O=C1NN=C(c2ccc3nc(Cc4ccccc4)oc3c2)C2CC12 nan
CHEMBL3922455 153282 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 3 1 4 2.9 O=C1NN=C(c2ccc3nc(Cc4ccccc4)oc3c2)C2CC12 nan
71546854 93017 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 475 5 0 9 3.9 Cc1c(Oc2ccc(-n3ccnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312514 93017 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 475 5 0 9 3.9 Cc1c(Oc2ccc(-n3ccnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
89995614 154123 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 504 5 0 4 6.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)C2CC2)CC1 nan
CHEMBL3929333 154123 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 504 5 0 4 6.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)C2CC2)CC1 nan
54591185 160938 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 503 9 1 7 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCN(C(C)CC)CC4)c3)oc2c1 nan
CHEMBL3985503 160938 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 503 9 1 7 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCN(C(C)CC)CC4)c3)oc2c1 nan
54591486 157979 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 7 1 7 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CN4CCOCC4)cc3)oc2c1 nan
CHEMBL3959856 157979 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 7 1 7 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CN4CCOCC4)cc3)oc2c1 nan
134152907 160108 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 499 5 2 9 5.0 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(C#N)cc3Cl)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3978259 160108 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 499 5 2 9 5.0 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(C#N)cc3Cl)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
54592032 155359 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCCCC4)cc3)oc2c1 nan
CHEMBL3939014 155359 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCCCC4)cc3)oc2c1 nan
72946092 111391 0 None -128 4 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR119 assessed as cAMP accumulationAgonist activity at rat GPR119 assessed as cAMP accumulation
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104879 111391 0 None -128 4 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR119 assessed as cAMP accumulationAgonist activity at rat GPR119 assessed as cAMP accumulation
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
54586779 68360 0 None -10 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 417 4 0 5 3.8 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771089 68360 0 None -10 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 417 4 0 5 3.8 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
71655092 97544 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 493 6 1 5 6.1 N#Cc1c(C(F)(F)F)cc(C2CC2)nc1Oc1cccc(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391614 97544 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 493 6 1 5 6.1 N#Cc1c(C(F)(F)F)cc(C2CC2)nc1Oc1cccc(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2013.04.014
51354343 68033 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3CO[C@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766203 68033 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3CO[C@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
145978481 170409 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 411 7 0 5 4.3 CC(C)(C)OC(=O)N1CCC(CCCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
CHEMBL4203871 170409 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 411 7 0 5 4.3 CC(C)(C)OC(=O)N1CCC(CCCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
67466093 155062 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@H]1C nan
CHEMBL3936670 155062 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@H]1C nan
68385332 93751 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 6 0 5 4.5 CC(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1021/ml300399u
CHEMBL2323591 93751 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 6 0 5 4.5 CC(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1021/ml300399u
58116588 192842 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 487 4 0 8 3.4 CN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
CHEMBL4871114 192842 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 487 4 0 8 3.4 CN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
68021959 162610 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 463 5 0 9 3.1 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4059986 162610 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 463 5 0 9 3.1 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
145964295 170745 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 387 8 0 3 5.5 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CCCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4207878 170745 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 387 8 0 3 5.5 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CCCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
118722570 122930 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3357994 122930 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
71452110 89821 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 501 5 1 8 3.5 C[S+]([O-])c1cc(F)c(NC(=O)C2=NOC3(CCN(c4nc(-c5ccccc5)no4)CC3)C2)cc1F 10.1021/jm301549a
CHEMBL2181671 89821 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 501 5 1 8 3.5 C[S+]([O-])c1cc(F)c(NC(=O)C2=NOC3(CCN(c4nc(-c5ccccc5)no4)CC3)C2)cc1F 10.1021/jm301549a
118720425 122681 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 452 4 1 4 5.5 Fc1cccc(CC2(C3CC3)NCc3cnc4c(-c5ccc(C(F)(F)F)cc5)cnn4c32)c1 10.1016/j.bmcl.2014.10.010
CHEMBL3354797 122681 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 452 4 1 4 5.5 Fc1cccc(CC2(C3CC3)NCc3cnc4c(-c5ccc(C(F)(F)F)cc5)cnn4c32)c1 10.1016/j.bmcl.2014.10.010
51030053 84191 1 None 23 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086680 84191 1 None 23 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
51030053 84191 1 None 23 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1021/jm300310c
CHEMBL2086680 84191 1 None 23 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1021/jm300310c
51030896 84204 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 428 6 0 10 2.4 C[C@@H]1CN(c2noc(C(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086694 84204 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 428 6 0 10 2.4 C[C@@H]1CN(c2noc(C(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
76310441 111808 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 486 4 0 6 4.3 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)cc(Cl)c32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113637 111808 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 486 4 0 6 4.3 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)cc(Cl)c32)CC1 10.1016/j.bmc.2014.01.028
145973632 169877 0 None -8 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 473 6 1 7 5.1 CC(C)COC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
CHEMBL4177039 169877 0 None -8 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 473 6 1 7 5.1 CC(C)COC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
53630450 68869 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 485 5 0 9 3.1 CS(=O)(=O)c1ccc(-n2ncc3c(OC4CCN(C(=O)OC5CCCC5)CC4)ncnc32)cc1 10.1016/j.bmcl.2011.03.007
CHEMBL1775174 68869 0 None -1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 485 5 0 9 3.1 CS(=O)(=O)c1ccc(-n2ncc3c(OC4CCN(C(=O)OC5CCCC5)CC4)ncnc32)cc1 10.1016/j.bmcl.2011.03.007
89995713 155635 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 464 4 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3C#N)c(F)c2)C2CC2)CC1 nan
CHEMBL3941335 155635 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 464 4 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3C#N)c(F)c2)C2CC2)CC1 nan
118711211 120705 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 468 6 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325843 120705 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 468 6 0 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711794 120820 0 None 8 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 520 7 0 11 2.7 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)C)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326685 120820 0 None 8 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 520 7 0 11 2.7 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3noc(C(C)C)n3)CC2)c1F 10.1016/j.bmcl.2014.06.071
57397675 77604 1 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 390 5 0 7 3.5 Cc1c(Oc2cncc(F)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951018 77604 1 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 390 5 0 7 3.5 Cc1c(Oc2cncc(F)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
62706192 83002 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 422 6 1 5 4.2 CC(C)(C)OC(=O)N1CCC(CCCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058389 83002 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 422 6 1 5 4.2 CC(C)(C)OC(=O)N1CCC(CCCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
145985036 172445 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 543 5 2 10 3.9 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1C[C@H]2Nc1ncnc2c(Nc3ccc(S(C)(=O)=O)cc3F)ncnc12 10.1016/j.bmc.2018.06.035
CHEMBL4244655 172445 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 543 5 2 10 3.9 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1C[C@H]2Nc1ncnc2c(Nc3ccc(S(C)(=O)=O)cc3F)ncnc12 10.1016/j.bmc.2018.06.035
46885051 14680 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 440 6 0 7 1.9 CCS(=O)(=O)N1CCN(c2ccc(OC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1090169 14680 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 440 6 0 7 1.9 CCS(=O)(=O)N1CCN(c2ccc(OC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
46884989 15154 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 460 8 0 6 1.8 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)C(F)F)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1093190 15154 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 460 8 0 6 1.8 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)C(F)F)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
145964999 170948 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 8 4.2 CCc1cnc(N2CCC(c3nc(COc4c(F)cc(/C=C5\CC(=O)NC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4210487 170948 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 8 4.2 CCc1cnc(N2CCC(c3nc(COc4c(F)cc(/C=C5\CC(=O)NC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
51030896 84204 0 None -10 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 428 6 0 10 2.4 C[C@@H]1CN(c2noc(C(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086694 84204 0 None -10 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 428 6 0 10 2.4 C[C@@H]1CN(c2noc(C(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
145951687 169736 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 508 6 0 9 4.1 N#Cc1ccc(Oc2ncnc(OC3C4COCC3CN(c3ncc(F)cn3)C4)c2C2CC2)c(Cl)c1 10.1021/acsmedchemlett.8b00073
CHEMBL4174762 169736 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 508 6 0 9 4.1 N#Cc1ccc(Oc2ncnc(OC3C4COCC3CN(c3ncc(F)cn3)C4)c2C2CC2)c(Cl)c1 10.1021/acsmedchemlett.8b00073
71655017 97543 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 453 5 1 5 5.2 N#Cc1ccc(C(F)(F)F)nc1Oc1cccc(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391613 97543 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 453 5 1 5 5.2 N#Cc1ccc(C(F)(F)F)nc1Oc1cccc(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2013.04.014
76316928 110013 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 484 6 0 7 3.9 Cc1c(Oc2cccnc2C(F)(F)F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084380 110013 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 484 6 0 7 3.9 Cc1c(Oc2cccnc2C(F)(F)F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
67466151 149272 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 2.7 CO[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3890496 149272 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 2.7 CO[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
118720420 122676 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 480 5 0 6 4.9 CCOC(=O)C1(Cc2ccccc2)c2c(cnc3c(-c4ccc(C(F)(F)F)cc4)cnn23)CN1C 10.1016/j.bmcl.2014.10.010
CHEMBL3354792 122676 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 480 5 0 6 4.9 CCOC(=O)C1(Cc2ccccc2)c2c(cnc3c(-c4ccc(C(F)(F)F)cc4)cnn23)CN1C 10.1016/j.bmcl.2014.10.010
90001649 154052 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cccs3)cc2)C2CC2)CC1 nan
CHEMBL3928745 154052 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cccs3)cc2)C2CC2)CC1 nan
118722575 122935 0 None -14 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 463 5 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2F)cn1 10.1021/jm5011012
CHEMBL3357999 122935 0 None -14 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 463 5 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2F)cn1 10.1021/jm5011012
89670659 158025 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 474 8 1 6 5.2 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN5CCCCC5)cc4)oc3c2)[C@H]1C nan
CHEMBL3960172 158025 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 474 8 1 6 5.2 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN5CCCCC5)cc4)oc3c2)[C@H]1C nan
89995520 154523 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 447 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2c(F)cc(-c3cnco3)cc2F)C2CC2)CC1 nan
CHEMBL3932347 154523 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 447 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2c(F)cc(-c3cnco3)cc2F)C2CC2)CC1 nan
24822706 68340 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 422 3 0 5 4.0 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771068 68340 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 422 3 0 5 4.0 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
71547007 92959 6 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 506 5 0 10 3.6 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312158 92959 6 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 506 5 0 10 3.6 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
54589390 167399 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C(C)C)C(C)C)cc3)oc2c1 nan
CHEMBL4113048 167399 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C(C)C)C(C)C)cc3)oc2c1 nan
118711776 120802 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 494 7 0 9 3.4 CCC1(OC(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)CC1 10.1016/j.bmcl.2014.06.071
CHEMBL3326668 120802 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 494 7 0 9 3.4 CCC1(OC(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)CC1 10.1016/j.bmcl.2014.06.071
67607375 90447 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 448 6 0 10 2.6 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)CC1 10.1021/ml300296q
CHEMBL2204983 90447 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 448 6 0 10 2.6 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)CC1 10.1021/ml300296q
127048822 147772 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 426 6 0 6 4.2 CC(C)CCN1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823489 147772 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 426 6 0 6 4.2 CC(C)CCN1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
54587592 69005 0 None -3 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 466 6 0 7 3.4 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778255 69005 0 None -3 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 466 6 0 7 3.4 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
76313416 110021 0 None -14 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(C#N)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084388 110021 0 None -14 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(C#N)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
2661 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2012.12.013
5283454 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2012.12.013
CHEMBL280065 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2012.12.013
2661 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2017.03.092
5283454 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2017.03.092
CHEMBL280065 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2017.03.092
2661 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2016.10.030
5283454 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2016.10.030
CHEMBL280065 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2016.10.030
2661 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2012.12.011
5283454 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2012.12.011
CHEMBL280065 9630 65 None -4 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2012.12.011
58190395 84178 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 460 5 0 8 2.7 CC(C)(C)OC(=O)N1C[C@@H]2C[C@H]1CN2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086666 84178 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 460 5 0 8 2.7 CC(C)(C)OC(=O)N1C[C@@H]2C[C@H]1CN2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
89995559 153678 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 383 5 0 5 3.6 CCOC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3925590 153678 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 383 5 0 5 3.6 CCOC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
73387822 150048 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 6 3.5 Cn1cnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)n1 nan
CHEMBL3896809 150048 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 6 3.5 Cn1cnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)n1 nan
67466184 156886 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 459 7 1 8 4.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4nc(C(C)C)no4)cc3)oc2c1 nan
CHEMBL3951094 156886 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 459 7 1 8 4.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4nc(C(C)C)no4)cc3)oc2c1 nan
67464597 158637 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 1 4 3.1 O=C1NN=C(c2ccc3nc(-c4cccc(F)c4)oc3c2)C2CC12 nan
CHEMBL3965527 158637 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 1 4 3.1 O=C1NN=C(c2ccc3nc(-c4cccc(F)c4)oc3c2)C2CC12 nan
72945895 111397 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 515 6 1 6 5.3 Cc1cc2c(c(Sc3ccc(C)c(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104886 111397 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 515 6 1 6 5.3 Cc1cc2c(c(Sc3ccc(C)c(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
62706349 83004 0 None 1 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 408 5 1 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058391 83004 0 None 1 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 408 5 1 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
89995511 157720 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 428 4 2 7 2.9 CC1=NNNN1c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3957877 157720 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 428 4 2 7 2.9 CC1=NNNN1c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
145967591 171735 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 461 8 0 6 4.4 CCc1cnc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2F)C3)nc1 10.1016/j.bmc.2018.02.032
CHEMBL4225137 171735 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 461 8 0 6 4.4 CCc1cnc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2F)C3)nc1 10.1016/j.bmc.2018.02.032
67466124 156097 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 3 1 5 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3cc(C)cs3)oc2c1 nan
CHEMBL3944973 156097 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 3 1 5 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3cc(C)cs3)oc2c1 nan
60155183 84169 0 None -1 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 449 5 0 9 1.9 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
CHEMBL2086657 84169 0 None -1 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 449 5 0 9 1.9 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
67466408 157661 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccccn4)cc3)oc2c1 nan
CHEMBL3957426 157661 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccccn4)cc3)oc2c1 nan
162661226 188271 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 550 8 1 13 -0.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(OC)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4764779 188271 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 550 8 1 13 -0.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(OC)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
54584353 68008 0 None -3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None -3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
71457626 90440 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 504 5 0 5 5.0 CCc1cnc(N2CCC(C3Cc4cc(-c5ccc(C(=O)N6CC(F)(F)C6)cc5)ccc4O3)CC2)nc1 10.1021/ml300296q
CHEMBL2204976 90440 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 504 5 0 5 5.0 CCc1cnc(N2CCC(C3Cc4cc(-c5ccc(C(=O)N6CC(F)(F)C6)cc5)ccc4O3)CC2)nc1 10.1021/ml300296q
54584353 68008 0 None -3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None -3 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
89995613 152572 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 4 5.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccoc3)cc2)C2CC2)CC1 nan
CHEMBL3916931 152572 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 4 5.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccoc3)cc2)C2CC2)CC1 nan
67466873 149854 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 385 3 1 7 2.0 CCOC(=O)N1CCN(c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)CC1 nan
CHEMBL3895240 149854 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 385 3 1 7 2.0 CCOC(=O)N1CCN(c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)CC1 nan
118300932 154933 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 464 5 0 5 4.8 CN(C)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
CHEMBL3935553 154933 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 464 5 0 5 4.8 CN(C)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
127048820 147695 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 492 5 0 7 4.3 CC(C)(OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1)C(F)F 10.1016/j.bmcl.2016.06.050
CHEMBL3822488 147695 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 492 5 0 7 4.3 CC(C)(OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1)C(F)F 10.1016/j.bmcl.2016.06.050
140251511 172008 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 467 7 0 5 5.0 CS(=O)(=O)c1ccc(OCCCC2CC3(CCN(C(=O)OC4CCCC4)CC3)C2)cc1F 10.1016/j.bmc.2018.02.032
CHEMBL4229160 172008 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 467 7 0 5 5.0 CS(=O)(=O)c1ccc(OCCCC2CC3(CCN(C(=O)OC4CCCC4)CC3)C2)cc1F 10.1016/j.bmc.2018.02.032
127048820 147695 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 492 5 0 7 4.3 CC(C)(OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1)C(F)F 10.1016/j.bmc.2017.06.014
CHEMBL3822488 147695 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 492 5 0 7 4.3 CC(C)(OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1)C(F)F 10.1016/j.bmc.2017.06.014
72945706 111402 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 457 5 1 6 3.9 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104891 111402 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 457 5 1 6 3.9 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C)C2=O 10.1016/j.bmcl.2013.11.053
11705608 7224 65 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activationAgonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activation
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
12151 7224 65 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activationAgonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activation
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
CHEMBL1775179 7224 65 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activationAgonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activation
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
118720404 122660 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)c(C)nn12 10.1016/j.bmcl.2014.10.010
CHEMBL3354776 122660 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)c(C)nn12 10.1016/j.bmcl.2014.10.010
54583896 68368 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771097 68368 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
56943106 90444 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assayAgonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assay
ChEMBL 489 6 1 8 4.2 CN(C)C(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)(C)F)no4)CC3)c2F)c(F)c1 10.1021/ml300296q
CHEMBL2204980 90444 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assayAgonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assay
ChEMBL 489 6 1 8 4.2 CN(C)C(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)(C)F)no4)CC3)c2F)c(F)c1 10.1021/ml300296q
66963587 117544 0 None -4 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 454 6 0 6 4.9 CCOC(=O)[C@](C)(Cc1ccccc1)c1cnnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260540 117544 0 None -4 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 454 6 0 6 4.9 CCOC(=O)[C@](C)(Cc1ccccc1)c1cnnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
68209285 149250 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 486 6 1 6 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(O[C@H]4CCC[C@@H]4N4CCCCC4)cc3)oc2c1 nan
CHEMBL3890321 149250 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 486 6 1 6 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(O[C@H]4CCC[C@@H]4N4CCCCC4)cc3)oc2c1 nan
71736719 140493 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 397 2 0 5 5.1 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccncc4F)ncc3o2)CC1 nan
CHEMBL3715053 140493 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 397 2 0 5 5.1 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccncc4F)ncc3o2)CC1 nan
89995545 154370 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 514 5 1 7 4.3 CN(C)C(=O)Nc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)s1 nan
CHEMBL3931023 154370 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 514 5 1 7 4.3 CN(C)C(=O)Nc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)s1 nan
57390604 77612 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 449 6 1 9 2.7 Cc1nc(S(C)(=O)=O)ccc1Nc1cc(OC2CCN(C(=O)OC(C)C)CC2)ncn1 10.1016/j.bmcl.2011.12.092
CHEMBL1951027 77612 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 449 6 1 9 2.7 Cc1nc(S(C)(=O)=O)ccc1Nc1cc(OC2CCN(C(=O)OC(C)C)CC2)ncn1 10.1016/j.bmcl.2011.12.092
168288185 198537 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 378 5 0 10 1.3 Cc1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmc.2022.116614
CHEMBL5197666 198537 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 378 5 0 10 1.3 Cc1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmc.2022.116614
58190401 84202 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 392 5 0 10 1.7 Cc1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1021/jm300310c
CHEMBL2086692 84202 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 392 5 0 10 1.7 Cc1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1021/jm300310c
140254089 173779 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 520 6 0 6 5.2 CCOC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4288041 173779 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 520 6 0 6 5.2 CCOC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
57392378 77600 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1cc(S(C)(=O)=O)cnc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951013 77600 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1cc(S(C)(=O)=O)cnc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
68209580 160324 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4[C@@H](C)CC[C@@H]4C)cc3)oc2c1 nan
CHEMBL3980084 160324 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4[C@@H](C)CC[C@@H]4C)cc3)oc2c1 nan
70684960 84604 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 412 6 1 3 3.8 C[C@@H](CNC(=O)Cc1c(F)ccc(F)c1F)C1CCN(C(=O)OC2(C)CC2)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL2092875 84604 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 412 6 1 3 3.8 C[C@@H](CNC(=O)Cc1c(F)ccc(F)c1F)C1CCN(C(=O)OC2(C)CC2)CC1 10.1016/j.bmcl.2011.01.088
137650572 164214 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 522 6 2 10 3.5 CC(C)(C)OC(=O)N1CC2CC(Nc3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
CHEMBL4078851 164214 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 522 6 2 10 3.5 CC(C)(C)OC(=O)N1CC2CC(Nc3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
60155460 84193 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 399 4 0 7 3.2 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)C[C@H]2C)nc1 10.1021/jm300310c
CHEMBL2086683 84193 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 399 4 0 7 3.2 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)C[C@H]2C)nc1 10.1021/jm300310c
73387918 153449 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 422 4 0 5 4.1 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccnnc3)cc2)C2CC2)CC1 nan
CHEMBL3923763 153449 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 422 4 0 5 4.1 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccnnc3)cc2)C2CC2)CC1 nan
67461245 152311 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 448 7 1 7 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCOCC4)cc3)oc2c1 nan
CHEMBL3914989 152311 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 448 7 1 7 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCOCC4)cc3)oc2c1 nan
54591871 158404 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 2 1 4 3.6 C[C@@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@@H]1C nan
CHEMBL3963725 158404 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 2 1 4 3.6 C[C@@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@@H]1C nan
72945897 111395 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 485 6 1 6 4.6 Cc1cc2c(c(Oc3cccc(S(=O)(=O)Nc4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104884 111395 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 485 6 1 6 4.6 Cc1cc2c(c(Oc3cccc(S(=O)(=O)Nc4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
89995609 154260 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 412 4 0 6 3.7 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ncon3)cc2)C2CC2)CC1 nan
CHEMBL3930385 154260 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 412 4 0 6 3.7 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ncon3)cc2)C2CC2)CC1 nan
145968103 171829 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 409 5 0 5 3.9 CC(C)(C)OC(=O)N1CCC2(CC1)CC2CCOc1ccc(S(C)(=O)=O)cc1 10.1016/j.bmc.2018.02.032
CHEMBL4226381 171829 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 409 5 0 5 3.9 CC(C)(C)OC(=O)N1CCC2(CC1)CC2CCOc1ccc(S(C)(=O)=O)cc1 10.1016/j.bmc.2018.02.032
25012528 68356 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4cnccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771084 68356 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4cnccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
118711788 120815 0 None -6 2 Rat 6.6 pEC50 = 6.6 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 474 6 0 8 2.5 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326680 120815 0 None -6 2 Rat 6.6 pEC50 = 6.6 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 474 6 0 8 2.5 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
25053115 195107 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 589 7 1 11 5.0 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(-c5cccc(C(F)(F)F)c5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL500750 195107 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 589 7 1 11 5.0 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(-c5cccc(C(F)(F)F)c5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
71655315 97531 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 504 7 1 7 6.2 CC(C)c1noc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391601 97531 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 504 7 1 7 6.2 CC(C)c1noc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)n1 10.1016/j.bmcl.2013.04.014
76327867 109998 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 5 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084364 109998 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 5 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
76320654 110007 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 430 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084374 110007 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 430 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
56832511 79847 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 475 6 0 6 3.3 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)[C@@H]1CCN(Cc2nc3ccccc3s2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010852 79847 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 475 6 0 6 3.3 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)[C@@H]1CCN(Cc2nc3ccccc3s2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
118720404 122660 0 None -1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)c(C)nn12 10.1016/j.bmcl.2014.10.010
CHEMBL3354776 122660 0 None -1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 467 6 0 5 5.8 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)c(C)nn12 10.1016/j.bmcl.2014.10.010
164624288 192809 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4870635 192809 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
118300924 149518 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 451 4 0 5 5.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)s3)cc2)C2CC2)CC1 nan
CHEMBL3892438 149518 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 451 4 0 5 5.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)s3)cc2)C2CC2)CC1 nan
54591646 167327 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 405 6 1 5 5.2 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)[C@@H]1C nan
CHEMBL4112510 167327 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 405 6 1 5 5.2 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)[C@@H]1C nan
118711791 120817 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 8 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3(F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326682 120817 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 8 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3(F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711782 120809 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326674 120809 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
68299305 120328 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 495 6 0 9 4.2 CCc1cnc(N2CCC(Oc3ncnc4c(-c5ccc(S(C)(=O)=O)cc5)csc34)CC2)nc1 10.1016/j.bmcl.2014.07.020
CHEMBL3321829 120328 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 495 6 0 9 4.2 CCc1cnc(N2CCC(Oc3ncnc4c(-c5ccc(S(C)(=O)=O)cc5)csc34)CC2)nc1 10.1016/j.bmcl.2014.07.020
145975897 170591 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 605 9 0 9 5.2 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)N(CC6CCOCC6)C5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4206175 170591 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 605 9 0 9 5.2 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)N(CC6CCOCC6)C5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
71519026 93115 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 452 7 1 7 3.5 CC(C)COC(=O)N1CCC(n2cc(CNc3ccc(S(C)(=O)=O)cc3F)cn2)CC1 10.1016/j.bmcl.2012.10.119
CHEMBL2313407 93115 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 452 7 1 7 3.5 CC(C)COC(=O)N1CCC(n2cc(CNc3ccc(S(C)(=O)=O)cc3F)cn2)CC1 10.1016/j.bmcl.2012.10.119
76324302 110024 0 None -6 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 428 6 0 7 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084392 110024 0 None -6 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 428 6 0 7 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
73387818 149966 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 1 4 4.1 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cn[nH]c3)cc2)C2CC2)CC1 nan
CHEMBL3896180 149966 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 1 4 4.1 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cn[nH]c3)cc2)C2CC2)CC1 nan
67466471 160295 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 510 7 1 7 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCN(S(C)(=O)=O)CC4)cc3)oc2c1 nan
CHEMBL3979839 160295 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 510 7 1 7 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCN(S(C)(=O)=O)CC4)cc3)oc2c1 nan
21897603 68602 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 505 4 0 9 2.7 CC(C)(C)OC(=O)N1CCC([S+]([O-])c2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773284 68602 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 505 4 0 9 2.7 CC(C)(C)OC(=O)N1CCC([S+]([O-])c2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
76321373 111801 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 468 4 1 7 2.6 CC(C)(C)OC(=O)N1CCC(C(O)COC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113630 111801 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 468 4 1 7 2.6 CC(C)(C)OC(=O)N1CCC(C(O)COC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
54591410 152690 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 375 6 1 5 4.3 C=CCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1 nan
CHEMBL3917876 152690 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 375 6 1 5 4.3 C=CCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1 nan
67464696 150190 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 434 8 1 6 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(C)C(C)C)c3)oc2c1 nan
CHEMBL3898061 150190 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 434 8 1 6 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(C)C(C)C)c3)oc2c1 nan
51030710 96978 0 None -70 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382416 96978 0 None -70 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
66964172 117543 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 459 5 0 5 4.9 CC(Cc1ccccc1)(c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12)S(C)(=O)=O 10.1016/j.bmcl.2014.03.023
CHEMBL3260539 117543 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 459 5 0 5 4.9 CC(Cc1ccccc1)(c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12)S(C)(=O)=O 10.1016/j.bmcl.2014.03.023
54591719 153324 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 303 2 1 4 3.0 O=C1NN=C(c2ccc3nc(-c4ccccc4)oc3c2)C2CC12 nan
CHEMBL3922754 153324 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 303 2 1 4 3.0 O=C1NN=C(c2ccc3nc(-c4ccccc4)oc3c2)C2CC12 nan
67463368 156973 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 423 6 1 4 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(CCc4ccccc4)cc3)oc2c1 nan
CHEMBL3951942 156973 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 423 6 1 4 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(CCc4ccccc4)cc3)oc2c1 nan
155516183 176806 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 445 5 0 6 4.8 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(C(=O)N(C)C)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4442686 176806 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 445 5 0 6 4.8 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(C(=O)N(C)C)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
51030984 84197 0 None -26 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086687 84197 0 None -26 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
51030984 84197 0 None -26 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086687 84197 0 None -26 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
54591794 153991 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.3 Cc1cccc(-c2nc3ccc(C4=NNC(=O)C5CC45)cc3o2)c1 nan
CHEMBL3928264 153991 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.3 Cc1cccc(-c2nc3ccc(C4=NNC(=O)C5CC45)cc3o2)c1 nan
145951687 169736 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 508 6 0 9 4.1 N#Cc1ccc(Oc2ncnc(OC3C4COCC3CN(c3ncc(F)cn3)C4)c2C2CC2)c(Cl)c1 10.1021/acsmedchemlett.8b00073
CHEMBL4174762 169736 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 508 6 0 9 4.1 N#Cc1ccc(Oc2ncnc(OC3C4COCC3CN(c3ncc(F)cn3)C4)c2C2CC2)c(Cl)c1 10.1021/acsmedchemlett.8b00073
67465346 160715 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 11 1 6 5.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(CC(C)C)CC(C)C)c3)oc2c1 nan
CHEMBL3983486 160715 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 11 1 6 5.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(CC(C)C)CC(C)C)c3)oc2c1 nan
118722577 122938 0 None -9 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358001 122938 0 None -9 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
25053044 179770 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 485 7 1 11 3.2 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C5CC5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL451798 179770 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 485 7 1 11 3.2 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C5CC5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
24958871 68344 0 None 13 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 386 3 0 4 4.8 CC(=O)c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771071 68344 0 None 13 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 386 3 0 4 4.8 CC(=O)c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
71491707 171813 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 455 6 0 5 4.8 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)cc1F)C2 10.1016/j.bmc.2018.02.032
CHEMBL4226193 171813 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 455 6 0 5 4.8 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)cc1F)C2 10.1016/j.bmc.2018.02.032
68040046 130791 0 None 10 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 469 5 1 8 3.8 CC1(OC(=O)N2CC3COCC(C2)C3Oc2cc(Nc3ccc(C#N)cc3Cl)ncn2)CC1 10.1016/j.bmcl.2015.09.047
CHEMBL3629596 130791 0 None 10 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 469 5 1 8 3.8 CC1(OC(=O)N2CC3COCC(C2)C3Oc2cc(Nc3ccc(C#N)cc3Cl)ncn2)CC1 10.1016/j.bmcl.2015.09.047
76331519 110011 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 506 6 0 8 4.8 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(Cl)s2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084378 110011 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 506 6 0 8 4.8 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(Cl)s2)c1C 10.1016/j.bmcl.2011.04.035
118720417 122673 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 466 5 1 6 4.9 CCOC(=O)[C@@]1(Cc2ccccc2)CNc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354789 122673 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 466 5 1 6 4.9 CCOC(=O)[C@@]1(Cc2ccccc2)CNc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
57399344 77607 0 None 7 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951021 77607 0 None 7 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
60155543 84236 0 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2nc(C3CC3)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2087085 84236 0 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2nc(C3CC3)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
76324977 111802 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 3.8 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3c2ccc(S(C)(=O)=O)c3F)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113631 111802 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 3.8 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3c2ccc(S(C)(=O)=O)c3F)CC1 10.1016/j.bmc.2014.01.028
76310440 111807 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 3.8 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)cc(F)c32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113636 111807 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 3.8 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)cc(F)c32)CC1 10.1016/j.bmc.2014.01.028
145962089 168889 0 None -4 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 446 5 1 7 3.5 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4161243 168889 0 None -4 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 446 5 1 7 3.5 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
118720417 122673 0 None -1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 466 5 1 6 4.9 CCOC(=O)[C@@]1(Cc2ccccc2)CNc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354789 122673 0 None -1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 466 5 1 6 4.9 CCOC(=O)[C@@]1(Cc2ccccc2)CNc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
155527157 177902 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 480 6 0 7 5.0 CC(O[C@H]1CC[C@]2(CCC(C)(C)CO2)CC1)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4458134 177902 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 480 6 0 7 5.0 CC(O[C@H]1CC[C@]2(CCC(C)(C)CO2)CC1)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
145986357 172017 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 432 5 0 10 2.1 N#Cc1cnccc1COc1cnc(N2CCN(c3nnc(C(F)(F)F)o3)CC2)nc1 10.1016/j.bmc.2018.04.004
CHEMBL4229220 172017 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 432 5 0 10 2.1 N#Cc1cnccc1COc1cnc(N2CCN(c3nnc(C(F)(F)F)o3)CC2)nc1 10.1016/j.bmc.2018.04.004
58017033 89838 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 6 0 8 3.3 CC(C)COC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181694 89838 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 6 0 8 3.3 CC(C)COC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
90665949 116059 0 None 15 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3218816 116059 0 None 15 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
53491715 129068 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 6 0 8 2.7 CC1(OC(=O)N2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598095 129068 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 6 0 8 2.7 CC1(OC(=O)N2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)CC1 10.1016/j.bmcl.2015.04.102
11751802 68595 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 472 4 1 9 3.0 CC(C)(C)OC(=O)N1CCC(Nc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773277 68595 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 472 4 1 9 3.0 CC(C)(C)OC(=O)N1CCC(Nc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
57401106 77611 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1cc(S(C)(=O)=O)ncc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951025 77611 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1cc(S(C)(=O)=O)ncc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
76316927 110009 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 486 7 0 7 3.9 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084376 110009 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 486 7 0 7 3.9 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
10003301 179766 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 439 7 0 11 2.5 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(-n4cncn4)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL451796 179766 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 439 7 0 11 2.5 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(-n4cncn4)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
4027 7267 59 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
ChEMBL 307 4 2 4 2.6 OCCNc1cc(C)nc(n1)c1ccc(cc1)Br 10.1016/j.bmc.2012.02.006
5332859 7267 59 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
ChEMBL 307 4 2 4 2.6 OCCNc1cc(C)nc(n1)c1ccc(cc1)Br 10.1016/j.bmc.2012.02.006
CHEMBL1956589 7267 59 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
ChEMBL 307 4 2 4 2.6 OCCNc1cc(C)nc(n1)c1ccc(cc1)Br 10.1016/j.bmc.2012.02.006
76335867 111798 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 451 4 1 5 3.2 CC(C)(C)OC(=O)N1CCC(CCNC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113627 111798 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 451 4 1 5 3.2 CC(C)(C)OC(=O)N1CCC(CCNC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
54587812 68347 0 None -3 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771075 68347 0 None -3 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
118711777 120803 0 None -7 2 Rat 5.6 pEC50 = 5.6 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 10 1.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326669 120803 0 None -7 2 Rat 5.6 pEC50 = 5.6 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 10 1.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
24896777 89293 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 8 3.0 CSC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177760 89293 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 8 3.0 CSC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
58017035 89306 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 516 6 0 10 3.6 Cc1nc(OC2CCN(c3nc(C(C)C)no3)CC2)c2c(n1)N(c1ccc(S(C)(=O)=O)cc1F)CC2 10.1021/jm301404a
CHEMBL2177774 89306 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 516 6 0 10 3.6 Cc1nc(OC2CCN(c3nc(C(C)C)no3)CC2)c2c(n1)N(c1ccc(S(C)(=O)=O)cc1F)CC2 10.1021/jm301404a
24897459 89319 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 464 5 0 8 2.7 CCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177787 89319 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 464 5 0 8 2.7 CCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
58017039 89829 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 461 5 0 9 2.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)nc2)CC1 10.1021/jm301404a
CHEMBL2181682 89829 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 461 5 0 9 2.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)nc2)CC1 10.1021/jm301404a
137633771 163193 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 490 4 0 9 3.8 Cc1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
CHEMBL4066674 163193 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 490 4 0 9 3.8 Cc1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
72188621 96973 0 None -19 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382411 96973 0 None -19 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
60155099 84167 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086654 84167 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
70682125 83006 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 1 6 3.6 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058395 83006 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 1 6 3.6 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
68040046 130791 0 None -10 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 469 5 1 8 3.8 CC1(OC(=O)N2CC3COCC(C2)C3Oc2cc(Nc3ccc(C#N)cc3Cl)ncn2)CC1 10.1016/j.bmcl.2015.09.047
CHEMBL3629596 130791 0 None -10 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 469 5 1 8 3.8 CC1(OC(=O)N2CC3COCC(C2)C3Oc2cc(Nc3ccc(C#N)cc3Cl)ncn2)CC1 10.1016/j.bmcl.2015.09.047
89995612 158064 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 464 6 0 4 5.8 CCOc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
CHEMBL3960486 158064 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 464 6 0 4 5.8 CCOc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
162666691 189151 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 534 7 1 12 0.2 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(C)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4785060 189151 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 534 7 1 12 0.2 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(C)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
54580684 68997 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 4 0 7 4.1 Cc1ncccc1Oc1ncnc(O[C@H]2CC3CC2N(C(=O)OC(C)(C)C)C3)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778135 68997 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 4 0 7 4.1 Cc1ncccc1Oc1ncnc(O[C@H]2CC3CC2N(C(=O)OC(C)(C)C)C3)c1C 10.1016/j.bmcl.2011.04.035
145968993 171749 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 465 6 0 5 5.5 CC(C)(C)OC(=O)N1CCC2(CCC(CCCOc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmc.2018.02.032
CHEMBL4225355 171749 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 465 6 0 5 5.5 CC(C)(C)OC(=O)N1CCC2(CCC(CCCOc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmc.2018.02.032
67465376 155453 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3939773 155453 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
71471779 120334 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 518 5 0 8 4.5 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3F)csc12)C1CCN(C(=O)OC2(C)CC2)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321837 120334 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 518 5 0 8 4.5 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3F)csc12)C1CCN(C(=O)OC2(C)CC2)CC1 10.1016/j.bmcl.2014.07.020
68036918 168946 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 447 5 0 7 3.6 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Oc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4162299 168946 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 447 5 0 7 3.6 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Oc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
76316923 109996 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 8 0 7 3.8 CCCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
CHEMBL3084362 109996 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 8 0 7 3.8 CCCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
25053041 195688 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 459 6 1 11 2.6 Cc1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL507711 195688 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 459 6 1 11 2.6 Cc1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
71519189 93118 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 450 4 0 7 3.1 CC(C)OC(=O)N1CCC(n2cc3c(n2)CN(c2ccc(S(C)(=O)=O)cc2F)C3)CC1 10.1016/j.bmcl.2012.10.119
CHEMBL2313410 93118 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 450 4 0 7 3.1 CC(C)OC(=O)N1CCC(n2cc3c(n2)CN(c2ccc(S(C)(=O)=O)cc2F)C3)CC1 10.1016/j.bmcl.2012.10.119
57390603 77605 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 397 5 0 8 3.2 Cc1c(Oc2cncc(C#N)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951019 77605 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 397 5 0 8 3.2 Cc1c(Oc2cncc(C#N)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
67466133 156859 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 4 4.0 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(Cl)c3)oc2c1 nan
CHEMBL3950822 156859 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 4 4.0 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(Cl)c3)oc2c1 nan
46884821 15255 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 420 8 0 7 2.5 COCCN1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1093969 15255 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 420 8 0 7 2.5 COCCN1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
76310438 111799 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 4.0 CC(CC1CCN(C(=O)OC(C)(C)C)CC1)OC(=O)N1CCc2cc(S(C)(=O)=O)ccc21 10.1016/j.bmc.2014.01.028
CHEMBL3113628 111799 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 4.0 CC(CC1CCN(C(=O)OC(C)(C)C)CC1)OC(=O)N1CCc2cc(S(C)(=O)=O)ccc21 10.1016/j.bmc.2014.01.028
155531204 178402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 438 5 0 7 3.9 CC1(C)C[C@]2(CC[C@H](OCc3nc(-c4ccc(S(C)(=O)=O)c(F)c4)no3)CC2)CO1 10.1016/j.bmcl.2019.07.004
CHEMBL4465577 178402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 438 5 0 7 3.9 CC1(C)C[C@]2(CC[C@H](OCc3nc(-c4ccc(S(C)(=O)=O)c(F)c4)no3)CC2)CO1 10.1016/j.bmcl.2019.07.004
70692694 83001 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 436 5 1 5 3.8 CC(C)(C)OC(=O)N1CCC(CCCC(=O)Nc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058388 83001 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 436 5 1 5 3.8 CC(C)(C)OC(=O)N1CCC(CCCC(=O)Nc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
53492593 129062 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 461 5 0 6 4.2 Cc1nc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)ccc1C(=O)N(C)C 10.1016/j.bmcl.2015.04.102
CHEMBL3598089 129062 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 461 5 0 6 4.2 Cc1nc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)ccc1C(=O)N(C)C 10.1016/j.bmcl.2015.04.102
62706519 83016 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CO3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058404 83016 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CO3)CC1 10.1016/j.bmcl.2012.05.117
71736415 141346 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 421 2 0 5 5.6 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C#N)c(F)c4)ncc3o2)CC1 nan
CHEMBL3718008 141346 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 421 2 0 5 5.6 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C#N)c(F)c4)ncc3o2)CC1 nan
60155364 84181 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 491 6 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(=O)(=O)N(C)C)cc2)cn1 10.1021/jm300310c
CHEMBL2086669 84181 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 491 6 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(=O)(=O)N(C)C)cc2)cn1 10.1021/jm300310c
54585040 68600 0 None -77 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 518 7 0 9 3.4 CCN(CC1CCN(C(=O)OC(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1F 10.1016/j.bmcl.2011.03.007
CHEMBL1773281 68600 0 None -77 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 518 7 0 9 3.4 CCN(CC1CCN(C(=O)OC(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1F 10.1016/j.bmcl.2011.03.007
54591796 152494 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 331 2 1 4 3.6 Cc1ccc(-c2nc3ccc(C4=NNC(=O)C5CC45)cc3o2)cc1C nan
CHEMBL3916314 152494 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 331 2 1 4 3.6 Cc1ccc(-c2nc3ccc(C4=NNC(=O)C5CC45)cc3o2)cc1C nan
53630396 68596 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 486 5 1 9 3.3 CC(C)(C)OC(=O)N1CCC(CNc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773278 68596 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 486 5 1 9 3.3 CC(C)(C)OC(=O)N1CCC(CNc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
51029964 84186 0 None -5 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 463 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cn2)cn1 10.1021/jm300310c
CHEMBL2086674 84186 0 None -5 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 463 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cn2)cn1 10.1021/jm300310c
118711210 120704 0 None -1 2 Rat 6.6 pEC50 = 6.6 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 467 6 1 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325842 120704 0 None -1 2 Rat 6.6 pEC50 = 6.6 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 467 6 1 9 2.9 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
53492467 129055 0 None 5 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598082 129055 0 None 5 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
127048480 147786 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 458 5 0 8 3.8 CC(C)OC(=O)N1CCC(n2ncc3cc(Oc4cccc(S(C)(=O)=O)c4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823744 147786 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 458 5 0 8 3.8 CC(C)OC(=O)N1CCC(n2ncc3cc(Oc4cccc(S(C)(=O)=O)c4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
70682125 83006 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 1 6 3.6 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058395 83006 0 None -1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 1 6 3.6 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
53317209 65330 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 428 6 1 7 2.6 CC(CNC(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684030 65330 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 428 6 1 7 2.6 CC(CNC(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
122184150 129089 0 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
CHEMBL3598115 129089 0 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
67466062 153620 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 2 1 5 3.4 CC1CC(=O)NN=C1c1ccc2nc(-c3ccsc3)oc2c1 nan
CHEMBL3925080 153620 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 2 1 5 3.4 CC1CC(=O)NN=C1c1ccc2nc(-c3ccsc3)oc2c1 nan
122194421 130793 0 None 5 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 3.2 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2015.09.047
CHEMBL3629598 130793 0 None 5 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 3.2 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2015.09.047
62706355 83008 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 3 6 3.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)NNS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058397 83008 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 3 6 3.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)NNS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
56963355 90277 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assayAgonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assay
ChEMBL 475 6 2 8 3.8 CNC(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)(C)F)no4)CC3)c2F)c(F)c1 10.1021/ml300296q
CHEMBL2203304 90277 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assayAgonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assay
ChEMBL 475 6 2 8 3.8 CNC(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)(C)F)no4)CC3)c2F)c(F)c1 10.1021/ml300296q
127048482 147782 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 460 4 0 7 3.8 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823669 147782 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 460 4 0 7 3.8 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
137637873 163003 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 484 6 1 8 4.1 CCNC(=O)c1c(C)cc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1C 10.1016/j.bmc.2017.06.014
CHEMBL4064583 163003 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 484 6 1 8 4.1 CCNC(=O)c1c(C)cc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1C 10.1016/j.bmc.2017.06.014
145976366 170549 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 385 8 0 2 6.5 CN(C)C(=O)c1ccc(OCCCCCC2CCC3(CCCCC3)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4205711 170549 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 385 8 0 2 6.5 CN(C)C(=O)c1ccc(OCCCCCC2CCC3(CCCCC3)CC2)cc1 10.1016/j.bmcl.2018.02.044
118722577 122938 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358001 122938 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
118720409 122665 0 None -3 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 479 5 0 5 5.8 CCOC(=O)[C@@]1(Cc2ccccc2)CCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354781 122665 0 None -3 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 479 5 0 5 5.8 CCOC(=O)[C@@]1(Cc2ccccc2)CCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
155539620 179636 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4515029 179636 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
155538763 180049 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 506 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@@]2(CC1)CC(F)(F)CCO2)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4525262 180049 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 506 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@@]2(CC1)CC(F)(F)CCO2)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
89995719 160781 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 446 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3C#N)cc2)C2CC2)CC1 nan
CHEMBL3984023 160781 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 446 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3C#N)cc2)C2CC2)CC1 nan
67464700 167662 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 326 2 1 6 2.5 CC[C@H]1OC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
CHEMBL4115113 167662 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 326 2 1 6 2.5 CC[C@H]1OC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
164609135 191224 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 522 5 0 8 3.9 CC(C)(C)OC(=O)N1CCC(N(c2cc(O[C@H]3CC[C@H](S(C)(=O)=O)CC3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
CHEMBL4846489 191224 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 522 5 0 8 3.9 CC(C)(C)OC(=O)N1CCC(N(c2cc(O[C@H]3CC[C@H](S(C)(=O)=O)CC3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
71654939 97536 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 413 5 1 5 4.8 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391606 97536 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 413 5 1 5 4.8 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
76324932 111713 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 533 6 0 8 5.5 N#Cc1ccccc1S(=O)(=O)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113005 111713 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 533 6 0 8 5.5 N#Cc1ccccc1S(=O)(=O)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76335830 111729 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 538 7 0 8 5.6 COc1cc(-c2nc(C3CC3)no2)cc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)n1 10.1016/j.bmcl.2013.12.127
CHEMBL3113207 111729 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 538 7 0 8 5.6 COc1cc(-c2nc(C3CC3)no2)cc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CCC3)n1 10.1016/j.bmcl.2013.12.127
62706349 83004 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 408 5 1 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058391 83004 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 408 5 1 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
57402128 77366 0 None -50 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 400 5 0 7 4.0 Cc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
CHEMBL1949674 77366 0 None -50 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 400 5 0 7 4.0 Cc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
62706691 83017 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 388 5 1 5 4.5 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CCO3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058405 83017 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 388 5 1 5 4.5 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CCO3)CC1 10.1016/j.bmcl.2012.05.117
71546701 93015 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 451 4 0 7 4.3 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312512 93015 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 451 4 0 7 4.3 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71655096 97466 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 443 6 2 6 4.2 Cc1cc(C(=O)O)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391432 97466 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 443 6 2 6 4.2 Cc1cc(C(=O)O)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
54591957 157519 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 427 6 1 7 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ncccn4)cc3)oc2c1 nan
CHEMBL3956328 157519 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 427 6 1 7 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ncccn4)cc3)oc2c1 nan
68036951 169630 0 None -14 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 513 6 1 10 3.1 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(-n4cncn4)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4172962 169630 0 None -14 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 513 6 1 10 3.1 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(-n4cncn4)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
118300919 151945 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 409 4 0 4 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cccc3)cc2)C2CC2)CC1 nan
CHEMBL3912264 151945 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 409 4 0 4 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cccc3)cc2)C2CC2)CC1 nan
86694583 140756 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 483 5 0 5 4.4 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(CC5(C(F)(F)F)CC5)CC4)oc3cn2)CC1 nan
CHEMBL3715997 140756 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 483 5 0 5 4.4 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(CC5(C(F)(F)F)CC5)CC4)oc3cn2)CC1 nan
68211912 117674 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 554 10 1 7 4.2 CCCc1cnc(N2CCC(C3(C)Cc4cc(C5=CCN(S(=O)(=O)CCCCO)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261143 117674 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 554 10 1 7 4.2 CCCc1cnc(N2CCC(C3(C)Cc4cc(C5=CCN(S(=O)(=O)CCCCO)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
90665949 116059 0 None 15 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm5011012
CHEMBL3218816 116059 0 None 15 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm5011012
68240419 130774 0 None -5 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629481 130774 0 None -5 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
118722585 122948 0 None -7 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 564 7 0 10 2.5 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358011 122948 0 None -7 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 564 7 0 10 2.5 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
56963356 90445 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assayAgonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assay
ChEMBL 461 6 2 8 3.6 CC(C)(F)c1noc(C2CCN(c3ncnc(Nc4ccc(C(N)=O)cc4F)c3F)CC2)n1 10.1021/ml300296q
CHEMBL2204981 90445 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assayAgonist activity at GPR119 expressed in CHO-K1 cells assessed as cAMP level after 1 hr by homogenous time-resolved fluorescence assay
ChEMBL 461 6 2 8 3.6 CC(C)(F)c1noc(C2CCN(c3ncnc(Nc4ccc(C(N)=O)cc4F)c3F)CC2)n1 10.1021/ml300296q
68230201 129065 0 None 1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 402 4 0 7 3.5 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(C#N)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598092 129065 0 None 1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 402 4 0 7 3.5 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(C#N)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
68230212 129072 0 None -2 3 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598099 129072 0 None -2 3 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
122194337 130771 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
CHEMBL3629478 130771 0 None -3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.6 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
46884987 15020 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 480 8 0 6 3.0 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)CC(C)(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1092334 15020 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 480 8 0 6 3.0 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)CC(C)(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
71736569 141034 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 421 2 0 5 5.6 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C#N)cc4F)ncc3o2)CC1 nan
CHEMBL3716935 141034 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 421 2 0 5 5.6 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C#N)cc4F)ncc3o2)CC1 nan
164622064 193014 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 531 7 0 9 3.4 COCCN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
CHEMBL4873459 193014 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 531 7 0 9 3.4 COCCN(c1cc(N2CCc3cc(S(C)(=O)=O)ccc32)ncn1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
76684033 171914 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 460 7 0 4 5.3 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N3CCCC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4227731 171914 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 460 7 0 4 5.3 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N3CCCC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
145976269 170373 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 389 8 0 4 4.7 CN(C)C(=O)c1ccc(OCCCCCC2CCC3(CC2)OCCCO3)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4203517 170373 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 389 8 0 4 4.7 CN(C)C(=O)c1ccc(OCCCCCC2CCC3(CC2)OCCCO3)cc1 10.1016/j.bmcl.2018.02.044
11503692 77598 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1021/jm301626p
CHEMBL1951011 77598 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1021/jm301626p
70683090 79838 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 476 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C[C@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010844 79838 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 476 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C[C@H]1F 10.1016/j.bmcl.2011.10.033
70683091 79840 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 488 7 0 7 3.0 CO[C@@H]1CN(Cc2ccc(C(F)(F)F)cc2)CC[C@@H]1N(C)C(=O)Cc1ccc(-n2cnnn2)cc1 10.1016/j.bmcl.2011.10.033
CHEMBL2010846 79840 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 488 7 0 7 3.0 CO[C@@H]1CN(Cc2ccc(C(F)(F)F)cc2)CC[C@@H]1N(C)C(=O)Cc1ccc(-n2cnnn2)cc1 10.1016/j.bmcl.2011.10.033
60155274 84180 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 469 5 0 8 2.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCC2CCN(S(C)(=O)=O)CC2)cn1 10.1021/jm300310c
CHEMBL2086668 84180 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 469 5 0 8 2.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCC2CCN(S(C)(=O)=O)CC2)cn1 10.1021/jm300310c
155514929 176716 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 480 6 0 7 5.0 CC(O[C@H]1CC[C@@]2(CC1)CC(C)(C)CCO2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4441437 176716 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 480 6 0 7 5.0 CC(O[C@H]1CC[C@@]2(CC1)CC(C)(C)CCO2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
118711779 120806 0 None 11 2 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 550 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326671 120806 0 None 11 2 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 550 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
76314045 111712 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 508 6 0 7 5.6 O=S(=O)(c1ccccc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113004 111712 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 508 6 0 7 5.6 O=S(=O)(c1ccccc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
66964621 117521 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 391 5 0 5 4.7 CCOC(=O)C(c1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260513 117521 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 391 5 0 5 4.7 CCOC(=O)C(c1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
76320657 110017 0 None -5 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 474 6 0 7 4.0 Cc1c(Oc2ccc(Cl)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084384 110017 0 None -5 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 474 6 0 7 4.0 Cc1c(Oc2ccc(Cl)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
67467141 159865 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C(C)OC)cc3)oc2c1 nan
CHEMBL3976133 159865 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C(C)OC)cc3)oc2c1 nan
122184146 129085 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 7 0 7 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598111 129085 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 7 0 7 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
89995537 152428 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 0 5 5.9 Cc1c(-c2ccccc2)ncn1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3915823 152428 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 0 5 5.9 Cc1c(-c2ccccc2)ncn1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
67466236 149963 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 8 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCCN4CCCCC4)cc3)oc2c1 nan
CHEMBL3896160 149963 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 8 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCCN4CCCCC4)cc3)oc2c1 nan
67464584 159652 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)c(F)c3)oc2c1 nan
CHEMBL3974403 159652 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)c(F)c3)oc2c1 nan
71655176 97469 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 470 6 1 6 4.2 Cc1cc(C(=O)N(C)C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391435 97469 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 470 6 1 6 4.2 Cc1cc(C(=O)N(C)C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
54591568 151180 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 6 2 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4)cc3)oc2c1 nan
CHEMBL3906059 151180 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 6 2 6 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4)cc3)oc2c1 nan
67464826 151464 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 6 2 6 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CO)cc3)oc2c1 nan
CHEMBL3908462 151464 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 6 2 6 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CO)cc3)oc2c1 nan
67461955 156566 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 6 1 6 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4C)cc3)oc2c1 nan
CHEMBL3948480 156566 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 6 1 6 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4C)cc3)oc2c1 nan
118711789 120599 0 None -3 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 470 6 0 8 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325461 120599 0 None -3 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 470 6 0 8 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
118722573 122933 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 498 6 0 10 2.6 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm5011012
CHEMBL3357997 122933 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 498 6 0 10 2.6 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm5011012
118720422 122678 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 498 5 1 6 4.3 CCOC(=O)C1(Cc2cccc(F)c2)NC(=O)c2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354794 122678 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 498 5 1 6 4.3 CCOC(=O)C1(Cc2cccc(F)c2)NC(=O)c2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
89995550 157639 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 5 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cocn3)cc2)C2CC2)CC1 nan
CHEMBL3957214 157639 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 5 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cocn3)cc2)C2CC2)CC1 nan
72945710 111406 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 519 6 1 6 5.4 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(c1ccccc1)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104895 111406 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 519 6 1 6 5.4 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(c1ccccc1)C2=O 10.1016/j.bmcl.2013.11.053
67467279 150840 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 434 9 1 6 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(CC)CC)cc3)oc2c1 nan
CHEMBL3903194 150840 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 434 9 1 6 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(CC)CC)cc3)oc2c1 nan
54591571 167369 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 4 1 4 3.6 CCC[C@H]1C(=O)NN=C(c2ccc3nc(C4CC4)oc3c2)[C@@H]1C nan
CHEMBL4112778 167369 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 311 4 1 4 3.6 CCC[C@H]1C(=O)NN=C(c2ccc3nc(C4CC4)oc3c2)[C@@H]1C nan
68230212 129072 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598099 129072 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
54587813 68369 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771098 68369 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
71471711 120333 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 520 4 0 8 4.7 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3F)csc12)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321835 120333 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 520 4 0 8 4.7 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3F)csc12)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2014.07.020
53235503 110022 0 None 46 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 473 6 1 7 3.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084389 110022 0 None 46 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 473 6 1 7 3.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
71208637 90441 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 481 5 0 7 3.0 CS(=O)(=O)N1CC=C(c2cc3c(cn2)O[C@@H](C2CCN(c4ncc(C5CC5)cn4)CC2)C3)CC1 10.1021/ml300296q
CHEMBL2204977 90441 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 481 5 0 7 3.0 CS(=O)(=O)N1CC=C(c2cc3c(cn2)O[C@@H](C2CCN(c4ncc(C5CC5)cn4)CC2)C3)CC1 10.1021/ml300296q
71208866 90442 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 523 4 0 7 3.5 C[C@@]1(C2CCN(c3ncc(C(F)(F)F)cn3)CC2)Cc2cc(C3=CCN(S(C)(=O)=O)CC3)ncc2O1 10.1021/ml300296q
CHEMBL2204978 90442 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysisAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP concentration after 45 mins by Alphascreen analysis
ChEMBL 523 4 0 7 3.5 C[C@@]1(C2CCN(c3ncc(C(F)(F)F)cn3)CC2)Cc2cc(C3=CCN(S(C)(=O)=O)CC3)ncc2O1 10.1021/ml300296q
66964040 122661 0 None 2 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 487 6 0 5 6.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(Cl)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
CHEMBL3354777 122661 0 None 2 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 487 6 0 5 6.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(Cl)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
118720408 122664 0 None 2 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 469 4 0 5 5.2 COC(=O)[C@@]1(Cc2cccc(F)c2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354780 122664 0 None 2 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 469 4 0 5 5.2 COC(=O)[C@@]1(Cc2cccc(F)c2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
118720412 122668 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 431 5 0 5 5.0 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(Cl)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354784 122668 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 431 5 0 5 5.0 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(Cl)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
118720419 122675 0 None 4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 470 4 1 6 4.3 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354791 122675 0 None 4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 470 4 1 6 4.3 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
51029965 84184 0 None 11 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm300310c
CHEMBL2086672 84184 0 None 11 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm300310c
71128816 130519 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622176 130519 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
137634873 162923 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 519 6 1 10 3.7 CC(C)(C)OC(=O)N1CC2CCC1CC2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4063625 162923 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 519 6 1 10 3.7 CC(C)(C)OC(=O)N1CC2CCC1CC2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
90116115 130521 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 512 10 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(CC(=O)N4CCOCC4)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622178 130521 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 512 10 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(CC(=O)N4CCOCC4)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
122191630 130515 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622172 130515 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
70855957 162810 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 458 8 0 4 4.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)CC1 10.1016/j.bmcl.2017.01.091
CHEMBL4062339 162810 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 458 8 0 4 4.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)CC1 10.1016/j.bmcl.2017.01.091
71128816 130519 0 None -1 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622176 130519 0 None -1 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
25053253 183281 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 505 7 1 11 3.6 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)c(F)c4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL459682 183281 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 505 7 1 11 3.6 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)c(F)c4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
54585040 68600 0 None 77 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 518 7 0 9 3.4 CCN(CC1CCN(C(=O)OC(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1F 10.1016/j.bmcl.2011.03.007
CHEMBL1773281 68600 0 None 77 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 518 7 0 9 3.4 CCN(CC1CCN(C(=O)OC(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1F 10.1016/j.bmcl.2011.03.007
54581118 68604 0 None 25 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 489 4 0 8 3.5 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773287 68604 0 None 25 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 489 4 0 8 3.5 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1 10.1016/j.bmcl.2011.03.007
24996872 114314 84 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 456 7 0 8 4.0 CC(C)c1noc(N2CCC(COc3ccc(-c4ccc(S(C)(=O)=O)cc4)nc3)CC2)n1 10.1016/j.bmc.2018.06.035
CHEMBL3187503 114314 84 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 456 7 0 8 4.0 CC(C)c1noc(N2CCC(COc3ccc(-c4ccc(S(C)(=O)=O)cc4)nc3)CC2)n1 10.1016/j.bmc.2018.06.035
11224944 68866 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 459 5 0 9 2.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775171 68866 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 459 5 0 9 2.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
145959739 168996 0 None 19 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 471 5 1 7 4.9 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4162958 168996 0 None 19 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 471 5 1 7 4.9 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CC1 10.1021/acsmedchemlett.8b00073
134147816 156251 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 595 8 1 10 3.6 CS(=O)(=O)c1ccc(Nc2ncnc(OC3C[C@H]4CC[C@H](C3)N4S(=O)(=O)c3ccc(F)cc3)c2[N+](=O)[O-])c(F)c1 10.1016/j.bmc.2016.10.030
CHEMBL3946188 156251 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 595 8 1 10 3.6 CS(=O)(=O)c1ccc(Nc2ncnc(OC3C[C@H]4CC[C@H](C3)N4S(=O)(=O)c3ccc(F)cc3)c2[N+](=O)[O-])c(F)c1 10.1016/j.bmc.2016.10.030
164616327 191853 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 523 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(N(c2cc(OC3CCN(S(C)(=O)=O)CC3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
CHEMBL4855738 191853 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 523 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(N(c2cc(OC3CCN(S(C)(=O)=O)CC3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
71474456 130506 0 None 2 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 436 7 0 7 3.0 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622164 130506 0 None 2 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 436 7 0 7 3.0 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
90116115 130521 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 512 10 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(CC(=O)N4CCOCC4)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622178 130521 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 512 10 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(CC(=O)N4CCOCC4)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
53630415 68865 0 None 13 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 445 5 0 9 2.2 CCOC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775170 68865 0 None 13 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 445 5 0 9 2.2 CCOC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
71116044 130522 0 None -3 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 453 9 0 9 2.8 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622179 130522 0 None -3 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 453 9 0 9 2.8 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
164624288 192809 0 None -1 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR119 in GLUTag cells assessed as induction of GLP-1 secretion after 2 hrs by ELISAAgonist activity at rat GPR119 in GLUTag cells assessed as induction of GLP-1 secretion after 2 hrs by ELISA
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4870635 192809 0 None -1 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR119 in GLUTag cells assessed as induction of GLP-1 secretion after 2 hrs by ELISAAgonist activity at rat GPR119 in GLUTag cells assessed as induction of GLP-1 secretion after 2 hrs by ELISA
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
10166 9245 65 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2019.126855
25025505 9245 65 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2019.126855
CHEMBL3260505 9245 65 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2019.126855
DB12345 9245 65 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2019.126855
76314115 111681 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 490 6 0 7 3.6 CCc1cnc(N2CCC(C(C)COC(=O)N3CCc4cc(S(C)(=O)=O)cc(F)c43)CC2)nc1 10.1016/j.bmc.2014.01.028
CHEMBL3112602 111681 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 490 6 0 7 3.6 CCc1cnc(N2CCC(C(C)COC(=O)N3CCc4cc(S(C)(=O)=O)cc(F)c43)CC2)nc1 10.1016/j.bmc.2014.01.028
66964555 117540 0 None -38 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 496 8 0 5 5.0 COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260536 117540 0 None -38 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 496 8 0 5 5.0 COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
54583895 68366 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
CHEMBL1771095 68366 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
127048821 147721 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 447 4 0 7 4.0 Cc1ccc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
CHEMBL3822863 147721 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 447 4 0 7 4.0 Cc1ccc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
76314042 111705 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 478 5 0 6 4.7 COC(=O)c1cc(Cl)nc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CC3)c1 10.1016/j.bmcl.2013.12.127
CHEMBL3112997 111705 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 478 5 0 6 4.7 COC(=O)c1cc(Cl)nc(Oc2ccc3c(c2)N(S(=O)(=O)c2ccc(Cl)cc2)CC3)c1 10.1016/j.bmcl.2013.12.127
76328496 111719 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 533 6 0 8 5.5 N#Cc1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
CHEMBL3113011 111719 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 533 6 0 8 5.5 N#Cc1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
76316923 109996 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 8 0 7 3.8 CCCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
CHEMBL3084362 109996 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 8 0 7 3.8 CCCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
76316924 110004 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 5 0 7 4.3 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC2CCC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084370 110004 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 5 0 7 4.3 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC2CCC2)c1C 10.1016/j.bmcl.2011.04.035
71453941 89822 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 464 4 1 8 3.6 N#Cc1cc(F)c(NC(=O)C2=NOC3(CCN(c4nc(-c5ccccc5)no4)CC3)C2)cc1F 10.1021/jm301549a
CHEMBL2181672 89822 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 464 4 1 8 3.6 N#Cc1cc(F)c(NC(=O)C2=NOC3(CCN(c4nc(-c5ccccc5)no4)CC3)C2)cc1F 10.1021/jm301549a
118722581 122942 0 None -7 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358005 122942 0 None -7 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
89995643 149783 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@@H](F)C1 nan
CHEMBL3894640 149783 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@@H](F)C1 nan
67462531 167638 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)C)cc3)oc2c1 nan
CHEMBL4114940 167638 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)C)cc3)oc2c1 nan
122184150 129089 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
CHEMBL3598115 129089 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
118711781 120808 0 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 498 5 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326673 120808 0 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 498 5 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711798 120824 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 10 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3ncc(Cl)cn3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326689 120824 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 10 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3ncc(Cl)cn3)CC2)c1F 10.1016/j.bmcl.2014.06.071
58074125 191891 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 473 4 1 8 3.4 CC(C)(C)OC(=O)N1CCC(Nc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116208
CHEMBL4856239 191891 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 473 4 1 8 3.4 CC(C)(C)OC(=O)N1CCC(Nc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116208
71655254 97529 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 489 7 1 7 5.3 CCn1cnnc1-c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391599 97529 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 489 7 1 7 5.3 CCn1cnnc1-c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
71717324 93007 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 521 4 0 9 4.7 Cc1ncn(-c2ccc(Oc3ncnc(N4C5CC6CC4CC(C5)N6C(=O)OC(C)(C)C)c3C)c(F)c2)n1 10.1021/jm301626p
CHEMBL2312501 93007 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 521 4 0 9 4.7 Cc1ncn(-c2ccc(Oc3ncnc(N4C5CC6CC4CC(C5)N6C(=O)OC(C)(C)C)c3C)c(F)c2)n1 10.1021/jm301626p
46884859 14484 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 484 9 0 8 1.8 COCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1088853 14484 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 484 9 0 8 1.8 COCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
46884857 15145 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 468 7 0 7 2.6 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)C(C)C)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1093150 15145 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 468 7 0 7 2.6 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)C(C)C)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
46865203 15146 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 468 8 0 7 2.6 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1093151 15146 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 468 8 0 7 2.6 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
76335131 109997 0 None -5 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 426 4 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084363 109997 0 None -5 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 426 4 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
67466475 151401 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@H]2CCc3nc(-c4ccccc4)oc3C2)[C@@H]2C[C@H]12 nan
CHEMBL3908007 151401 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@H]2CCc3nc(-c4ccccc4)oc3C2)[C@@H]2C[C@H]12 nan
3800660 179900 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 451 7 1 10 1.6 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(S(N)(=O)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL452070 179900 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 451 7 1 10 1.6 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(S(N)(=O)=O)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
24939268 7240 67 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2014.03.023
5653 7240 67 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2014.03.023
CHEMBL461384 7240 67 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2014.03.023
155532104 178471 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 484 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2F)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4466588 178471 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 484 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2F)no1 10.1016/j.bmcl.2019.07.004
67465457 154893 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 489 8 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(C)C)CC4)cc3)oc2c1 nan
CHEMBL3935249 154893 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 489 8 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(C)C)CC4)cc3)oc2c1 nan
67466169 151880 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 7 1 6 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCCC4)c3)oc2c1 nan
CHEMBL3911754 151880 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 7 1 6 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCCC4)c3)oc2c1 nan
54591567 151086 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 5 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCCCCN4C)cc3)oc2c1 nan
CHEMBL3905322 151086 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 5 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCCCCN4C)cc3)oc2c1 nan
67462498 158194 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3961724 158194 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
60152410 147799 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 455 3 0 6 4.7 CC(C)(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ccc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823843 147799 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 455 3 0 6 4.7 CC(C)(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ccc32)CC1 10.1016/j.bmcl.2016.06.050
140251500 171753 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 469 7 0 5 5.1 CC(C)(C)COC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4225414 171753 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 469 7 0 5 5.1 CC(C)(C)COC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
76683715 171986 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 443 8 0 6 4.3 CCc1cnc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2)C3)nc1 10.1016/j.bmc.2018.02.032
CHEMBL4228905 171986 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 443 8 0 6 4.3 CCc1cnc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2)C3)nc1 10.1016/j.bmc.2018.02.032
68021864 165008 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 462 5 0 8 3.7 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)cc5)ccc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4088233 165008 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 462 5 0 8 3.7 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)cc5)ccc43)CC2)nc1 10.1016/j.bmc.2017.06.014
71655097 97467 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 508 8 2 6 5.0 N#Cc1c(C(=O)NC2CC2)cc(C2CC2)nc1Oc1cccc(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391433 97467 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 508 8 2 6 5.0 N#Cc1c(C(=O)NC2CC2)cc(C2CC2)nc1Oc1cccc(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2013.04.014
11641004 77641 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 452 6 1 8 3.2 CC(C)OC(=O)N1CCC(Oc2cc(Nc3ccc(S(C)(=O)=O)cc3F)ncn2)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951118 77641 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 452 6 1 8 3.2 CC(C)OC(=O)N1CCC(Oc2cc(Nc3ccc(S(C)(=O)=O)cc3F)ncn2)CC1 10.1016/j.bmcl.2011.12.092
24961798 68352 0 None -5 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cc(C#N)ncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771080 68352 0 None -5 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cc(C#N)ncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
155525764 177802 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 CC(O[C@H]1CC[C@@]2(CC1)CC(C)(C)CO2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4456673 177802 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 CC(O[C@H]1CC[C@@]2(CC1)CC(C)(C)CO2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
67462446 156423 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 5 3.3 CC1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3947320 156423 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 5 3.3 CC1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
53491782 129070 0 None 11 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598097 129070 0 None 11 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
24900244 89294 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 480 5 0 8 3.4 CCSC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177761 89294 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 480 5 0 8 3.4 CCSC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
71736572 140581 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 379 2 0 5 5.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccncc4)ncc3o2)CC1 nan
CHEMBL3715396 140581 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 379 2 0 5 5.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccncc4)ncc3o2)CC1 nan
137635337 162953 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 506 5 0 10 3.5 COc1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
CHEMBL4063942 162953 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 506 5 0 10 3.5 COc1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
1267327 97532 11 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 393 5 1 5 4.5 Cc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.04.014
1267327 97532 11 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 393 5 1 5 4.5 Cc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.12.127
CHEMBL2391602 97532 11 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 393 5 1 5 4.5 Cc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.04.014
CHEMBL2391602 97532 11 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 393 5 1 5 4.5 Cc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.12.127
76314041 111704 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 626 6 0 9 5.7 O=S1(=O)CCN(S(=O)(=O)c2ccc(Cl)cc2)c2cc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)c(Cl)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112996 111704 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 626 6 0 9 5.7 O=S1(=O)CCN(S(=O)(=O)c2ccc(Cl)cc2)c2cc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)c(Cl)cc21 10.1016/j.bmcl.2013.12.127
67463201 159266 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)N4CCCC4)cc3)oc2c1 nan
CHEMBL3971167 159266 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)N4CCCC4)cc3)oc2c1 nan
68036798 169220 0 None -6 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 501 7 1 9 3.0 COCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4166451 169220 0 None -6 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 501 7 1 9 3.0 COCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
141750310 186445 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 600 8 1 11 3.2 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(c3nc(-c4ccccc4)cs3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4743350 186445 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 600 8 1 11 3.2 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(c3nc(-c4ccccc4)cs3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
54591798 157269 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 291 2 1 4 3.1 O=C1CCC(c2ccc3nc(-c4ccccc4)oc3c2)=NN1 nan
CHEMBL3954402 157269 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 291 2 1 4 3.1 O=C1CCC(c2ccc3nc(-c4ccccc4)oc3c2)=NN1 nan
137643838 164845 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 505 6 1 10 3.3 CC(C)(C)OC(=O)N1CC2CC(Oc3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
CHEMBL4086187 164845 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 505 6 1 10 3.3 CC(C)(C)OC(=O)N1CC2CC(Oc3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
118711216 120711 0 None -4 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 472 6 0 9 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325849 120711 0 None -4 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 472 6 0 9 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
89995525 150798 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 6 4.0 Cc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)no1 nan
CHEMBL3902915 150798 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 6 4.0 Cc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)no1 nan
89995617 158066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 465 6 0 5 5.2 CCOc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
CHEMBL3960522 158066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 465 6 0 5 5.2 CCOc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
67464810 149471 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 349 4 1 5 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OC)c3)oc2c1 nan
CHEMBL3892085 149471 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 349 4 1 5 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OC)c3)oc2c1 nan
58017005 89292 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 494 7 0 9 2.3 COCCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177759 89292 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 494 7 0 9 2.3 COCCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
21897825 89300 26 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 126 0 1 3 -0.1 N#CN1CCC(O)CC1 10.1021/jm301404a
CHEMBL2177768 89300 26 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 126 0 1 3 -0.1 N#CN1CCC(O)CC1 10.1021/jm301404a
24897458 89318 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 450 4 0 8 2.3 COC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177786 89318 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 450 4 0 8 2.3 COC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
90666914 116237 0 None -6 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)O[C@@H]2CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220242 116237 0 None -6 2 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)O[C@@H]2CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
68230018 129069 0 None -8 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598096 129069 0 None -8 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
118292201 154931 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 445 4 0 4 5.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccccc3C#N)cc2)C2CC2)CC1 nan
CHEMBL3935545 154931 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 445 4 0 4 5.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccccc3C#N)cc2)C2CC2)CC1 nan
137655380 165476 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 461 8 0 7 4.0 CCc1cnc(N2CCC(COc3ccc(-c4ccc(C(=O)N(C)OC)cc4)nc3)CC2)nc1 10.1016/j.bmcl.2017.06.032
CHEMBL4093173 165476 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 461 8 0 7 4.0 CCc1cnc(N2CCC(COc3ccc(-c4ccc(C(=O)N(C)OC)cc4)nc3)CC2)nc1 10.1016/j.bmcl.2017.06.032
118722574 122934 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 512 7 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2)cn1 10.1021/jm5011012
CHEMBL3357998 122934 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 512 7 0 10 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2)cn1 10.1021/jm5011012
67463158 167221 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 488 8 1 6 5.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(O[C@@H]4CCCC[C@H]4N(CC)CC)cc3)oc2c1 nan
CHEMBL4111607 167221 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 488 8 1 6 5.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(O[C@@H]4CCCC[C@H]4N(CC)CC)cc3)oc2c1 nan
53318502 65337 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 400 6 1 3 3.7 CC(C)OC(=O)N1CCC(C(C)CNC(=O)Cc2c(F)ccc(F)c2F)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684037 65337 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 400 6 1 3 3.7 CC(C)OC(=O)N1CCC(C(C)CNC(=O)Cc2c(F)ccc(F)c2F)CC1 10.1016/j.bmcl.2011.01.088
76309732 110008 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 432 7 0 7 3.4 CCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
CHEMBL3084375 110008 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 432 7 0 7 3.4 CCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
73388329 149205 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 427 4 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cncs3)cc2)C2CC2)CC1 nan
CHEMBL3889992 149205 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 427 4 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cncs3)cc2)C2CC2)CC1 nan
76332171 111715 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 526 6 0 7 5.7 O=S(=O)(c1cccc(F)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113007 111715 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 526 6 0 7 5.7 O=S(=O)(c1cccc(F)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
2661 9630 65 None -4 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2018.06.035
5283454 9630 65 None -4 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2018.06.035
CHEMBL280065 9630 65 None -4 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmc.2018.06.035
145983970 172231 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 431 19 3 3 7.2 CCCCCCCC/C=C\CCCCCCCC(=O)NCCCc1ccc(O)c(O)c1 10.1016/j.bmc.2018.06.035
CHEMBL4239244 172231 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 431 19 3 3 7.2 CCCCCCCC/C=C\CCCCCCCC(=O)NCCCc1ccc(O)c(O)c1 10.1016/j.bmc.2018.06.035
145993111 173693 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 591 6 1 6 6.3 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5cccc(C(=O)O)c5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4286549 173693 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 591 6 1 6 6.3 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5cccc(C(=O)O)c5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
137643882 164917 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 481 5 0 6 4.9 CC(C)(C)OC(=O)N1CCC(COc2ccc(-c3ccc(C(=O)N4CCCCO4)cc3)nc2)CC1 10.1016/j.bmcl.2017.06.032
CHEMBL4087173 164917 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 481 5 0 6 4.9 CC(C)(C)OC(=O)N1CCC(COc2ccc(-c3ccc(C(=O)N4CCCCO4)cc3)nc2)CC1 10.1016/j.bmcl.2017.06.032
76309729 110000 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 398 5 0 7 3.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
CHEMBL3084366 110000 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 398 5 0 7 3.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
139437096 178347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 464 6 0 8 2.3 CN(C)C(=O)C1CN(c2ncc(N3CC[C@@H](Oc4ccc(-c5nccs5)cc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
CHEMBL4464856 178347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 464 6 0 8 2.3 CN(C)C(=O)C1CN(c2ncc(N3CC[C@@H](Oc4ccc(-c5nccs5)cc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
67463208 159935 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 416 6 1 7 4.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cnco4)cc3)oc2c1 nan
CHEMBL3976724 159935 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 416 6 1 7 4.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cnco4)cc3)oc2c1 nan
118711777 120803 0 None 7 2 Human 6.5 pEC50 = 6.5 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 10 1.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326669 120803 0 None 7 2 Human 6.5 pEC50 = 6.5 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 6 0 10 1.9 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
67467925 156307 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 2 5 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(O)c3)oc2c1 nan
CHEMBL3946541 156307 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 2 5 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(O)c3)oc2c1 nan
137661559 165862 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 486 5 1 7 4.1 CC(C)NC(=O)c1cc(F)c(-c2cc3nnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
CHEMBL4097347 165862 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 486 5 1 7 4.1 CC(C)NC(=O)c1cc(F)c(-c2cc3nnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
72946091 111392 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 519 6 1 6 5.3 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3Cl)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104880 111392 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 519 6 1 6 5.3 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3Cl)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
155551991 181909 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 456 5 1 6 4.9 Cc1c(Nc2ccc(C(=O)N(C)C)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4569726 181909 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 456 5 1 6 4.9 Cc1c(Nc2ccc(C(=O)N(C)C)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
66561292 147278 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assayAgonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assay
ChEMBL 400 7 1 6 4.4 CC(C)c1noc(N2CCC(CC(F)CNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1021/acs.jmedchem.5b01198
CHEMBL3809973 147278 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assayAgonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assay
ChEMBL 400 7 1 6 4.4 CC(C)c1noc(N2CCC(CC(F)CNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1021/acs.jmedchem.5b01198
66561292 147278 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assay
ChEMBL 400 7 1 6 4.4 CC(C)c1noc(N2CCC(CC(F)CNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1021/acs.jmedchem.5b01198
CHEMBL3809973 147278 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHOK1 cells assessed as increase in cellular cAMP levels after 30 mins by HTRF assay
ChEMBL 400 7 1 6 4.4 CC(C)c1noc(N2CCC(CC(F)CNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1021/acs.jmedchem.5b01198
68039954 130777 0 None -8 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 5 1 8 4.1 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629484 130777 0 None -8 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 5 1 8 4.1 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
58190314 84183 0 None -5 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 452 5 0 10 2.5 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2)cn1 10.1021/jm300310c
CHEMBL2086671 84183 0 None -5 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 452 5 0 10 2.5 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2)cn1 10.1021/jm300310c
11705608 7224 65 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
12151 7224 65 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
CHEMBL1775179 7224 65 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 10.1016/j.bmcl.2011.03.007
89995646 154000 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 5 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3928358 154000 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 5 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
53630423 68607 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2ncn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773290 68607 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2ncn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
66964295 117538 0 None -7 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260533 117538 0 None -7 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 453 6 0 5 5.5 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
76316925 110005 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 404 5 0 7 2.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(C)(=O)=O)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084371 110005 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 404 5 0 7 2.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(C)(=O)=O)c1C 10.1016/j.bmcl.2011.04.035
62706355 83008 0 None -1 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 3 6 3.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)NNS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058397 83008 0 None -1 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 410 5 3 6 3.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)NNS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
118300915 157998 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 427 4 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3nccs3)cc2)C2CC2)CC1 nan
CHEMBL3960001 157998 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 427 4 0 5 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3nccs3)cc2)C2CC2)CC1 nan
89995717 153006 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 491 6 1 4 5.0 CC(=O)NCc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
CHEMBL3920324 153006 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 491 6 1 4 5.0 CC(=O)NCc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
54591339 153177 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 419 5 1 6 4.3 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOCC4)cc3)oc2c1 nan
CHEMBL3921688 153177 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 419 5 1 6 4.3 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOCC4)cc3)oc2c1 nan
118711776 120802 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 494 7 0 9 3.4 CCC1(OC(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)CC1 10.1016/j.bmcl.2014.06.071
CHEMBL3326668 120802 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 494 7 0 9 3.4 CCC1(OC(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)CC1 10.1016/j.bmcl.2014.06.071
144479903 174120 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 591 6 1 6 6.3 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccc5C(=O)O)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4294437 174120 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 591 6 1 6 6.3 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccc5C(=O)O)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
67467119 154625 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 1 5 3.4 COc1cccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)c1 nan
CHEMBL3933044 154625 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 1 5 3.4 COc1cccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)c1 nan
24958872 68339 0 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 2 0 3 4.9 Cc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771067 68339 0 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 2 0 3 4.9 Cc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
89995711 157057 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 415 5 0 6 3.0 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cncn3)c(F)c2)C2CC2)CC1 nan
CHEMBL3952641 157057 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 415 5 0 6 3.0 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cncn3)c(F)c2)C2CC2)CC1 nan
140251533 171853 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 446 7 0 4 4.9 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N3CCC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4226885 171853 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 446 7 0 4 4.9 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N3CCC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
76320658 110020 0 None 23 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(F)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084387 110020 0 None 23 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(F)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
68211784 117660 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 535 6 0 5 5.1 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ccc(C(F)(F)F)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261129 117660 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 535 6 0 5 5.1 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ccc(C(F)(F)F)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
71547006 92958 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 494 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312157 92958 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 494 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
118720418 122674 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.6 COC(=O)C1(Cc2ccccc2)OCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354790 122674 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.6 COC(=O)C1(Cc2ccccc2)OCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
57399342 77599 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 466 6 1 8 3.5 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951012 77599 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 466 6 1 8 3.5 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
51029965 84184 0 None -11 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm300310c
CHEMBL2086672 84184 0 None -11 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm300310c
89995538 152358 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 446 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)nc3)cc2)C2CC2)CC1 nan
CHEMBL3915303 152358 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 446 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)nc3)cc2)C2CC2)CC1 nan
89995653 153976 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 423 5 0 5 4.5 O=C(OC1CCCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3928136 153976 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 423 5 0 5 4.5 O=C(OC1CCCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
53317210 65335 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 378 5 1 3 3.8 CC(CNC(=O)Cc1cccc(F)c1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684035 65335 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 378 5 1 3 3.8 CC(CNC(=O)Cc1cccc(F)c1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
66964658 117519 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 504 7 0 7 3.9 CCOC(=O)C(C)(CC1CCN(S(C)(=O)=O)CC1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260511 117519 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 504 7 0 7 3.9 CCOC(=O)C(C)(CC1CCN(S(C)(=O)=O)CC1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
24958871 68344 0 None -13 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 386 3 0 4 4.8 CC(=O)c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771071 68344 0 None -13 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 386 3 0 4 4.8 CC(=O)c1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
60155459 84192 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 407 4 0 7 2.8 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3c(F)cncc3F)cn2)CC1 10.1021/jm300310c
CHEMBL2086682 84192 0 None -2 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 407 4 0 7 2.8 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3c(F)cncc3F)cn2)CC1 10.1021/jm300310c
67466006 158554 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 6 1 6 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)N4CCCCC4)cc3)oc2c1 nan
CHEMBL3964929 158554 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 6 1 6 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)N4CCCCC4)cc3)oc2c1 nan
118711779 120806 0 None -11 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 550 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326671 120806 0 None -11 2 Rat 6.5 pEC50 = 6.5 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 550 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)COC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
57404926 166527 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 475 5 0 7 4.6 CCc1cnc(N2CCC(n3ncc4c(C)c(-c5ccc(S(C)(=O)=O)cc5)ccc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4104975 166527 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 475 5 0 7 4.6 CCc1cnc(N2CCC(n3ncc4c(C)c(-c5ccc(S(C)(=O)=O)cc5)ccc43)CC2)nc1 10.1016/j.bmc.2017.06.014
54591025 156895 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 314 2 1 6 1.5 CC1CC(=O)NN=C1c1ccc2nc(N3CCOCC3)oc2c1 nan
CHEMBL3951150 156895 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 314 2 1 6 1.5 CC1CC(=O)NN=C1c1ccc2nc(N3CCOCC3)oc2c1 nan
145985107 172655 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 499 5 2 10 3.4 CC(C)(C)OC(=O)N1CCC(Nc2ncnc3c(Nc4ccc(S(C)(=O)=O)cc4)ncnc23)CC1 10.1016/j.bmc.2018.06.035
CHEMBL4249284 172655 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 499 5 2 10 3.4 CC(C)(C)OC(=O)N1CCC(Nc2ncnc3c(Nc4ccc(S(C)(=O)=O)cc4)ncnc23)CC1 10.1016/j.bmc.2018.06.035
89995536 159959 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccsc3)cc2)C2CC2)CC1 nan
CHEMBL3976969 159959 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccsc3)cc2)C2CC2)CC1 nan
67467954 154193 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccncc4)cc3)oc2c1 nan
CHEMBL3929873 154193 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccncc4)cc3)oc2c1 nan
67464497 158513 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 295 2 1 5 2.9 CC1CC(=O)NN=C1c1ccc2nc(-c3ccco3)oc2c1 nan
CHEMBL3964561 158513 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 295 2 1 5 2.9 CC1CC(=O)NN=C1c1ccc2nc(-c3ccco3)oc2c1 nan
67466277 160325 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 316 2 1 6 2.0 O=C1CCC(c2ccc3nc(N4CCSCC4)oc3c2)=NN1 nan
CHEMBL3980087 160325 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 316 2 1 6 2.0 O=C1CCC(c2ccc3nc(N4CCSCC4)oc3c2)=NN1 nan
118300916 154539 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 6 4.0 Cc1noc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)n1 nan
CHEMBL3932502 154539 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 6 4.0 Cc1noc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)n1 nan
145970589 171771 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 428 7 0 5 4.6 Cc1ccc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2)C3)nc1 10.1016/j.bmc.2018.02.032
CHEMBL4225666 171771 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 428 7 0 5 4.6 Cc1ccc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2)C3)nc1 10.1016/j.bmc.2018.02.032
67465462 155783 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 431 6 1 6 5.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccsc4)cc3)oc2c1 nan
CHEMBL3942366 155783 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 431 6 1 6 5.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccsc4)cc3)oc2c1 nan
71134925 171912 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 447 8 0 7 4.5 CC(C)c1noc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2)C3)n1 10.1016/j.bmc.2018.02.032
CHEMBL4227707 171912 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 447 8 0 7 4.5 CC(C)c1noc(N2CCC3(CC2)CC(CCCOc2ccc(S(C)(=O)=O)cc2)C3)n1 10.1016/j.bmc.2018.02.032
118720426 122683 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 501 5 2 8 3.2 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)nc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354799 122683 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 501 5 2 8 3.2 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)nc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354802 122683 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 501 5 2 8 3.2 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)nc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
118720418 122674 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.6 COC(=O)C1(Cc2ccccc2)OCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354790 122674 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 453 4 0 6 4.6 COC(=O)C1(Cc2ccccc2)OCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
58190343 84176 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 C[C@H]1CN(C(=O)OC(C)(C)C)C[C@@H](C)N1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086664 84176 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 C[C@H]1CN(C(=O)OC(C)(C)C)C[C@@H](C)N1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
71655175 97468 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 498 6 2 6 5.0 Cc1cc(C(=O)NC(C)(C)C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391434 97468 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 498 6 2 6 5.0 Cc1cc(C(=O)NC(C)(C)C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
76324300 110012 0 None -8 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 484 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(F)cc2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084379 110012 0 None -8 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 484 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(F)cc2)c1C 10.1016/j.bmcl.2011.04.035
62706691 83017 0 None -1 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 388 5 1 5 4.5 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CCO3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058405 83017 0 None -1 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 388 5 1 5 4.5 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CCO3)CC1 10.1016/j.bmcl.2012.05.117
56961034 163111 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 491 4 1 9 4.0 CC(C)(C)OC(=O)N1CCC(c2noc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL4065753 163111 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 491 4 1 9 4.0 CC(C)(C)OC(=O)N1CCC(c2noc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
59234074 170350 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 397 6 0 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
CHEMBL4203182 170350 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 397 6 0 5 3.9 CC(C)(C)OC(=O)N1CCC(CCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
53491782 129070 0 None -11 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598097 129070 0 None -11 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
72946093 111389 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(F)cc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104861 111389 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(F)cc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
145983137 172292 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 491 4 1 9 4.5 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc3c(Nc4ccc(C#N)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4240810 172292 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 491 4 1 9 4.5 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc3c(Nc4ccc(C#N)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
145964295 170904 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 387 8 0 3 5.5 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CCCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4209951 170904 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 387 8 0 3 5.5 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CCCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
24822706 68340 0 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 422 3 0 5 4.0 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771068 68340 0 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 422 3 0 5 4.0 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
54581962 68370 0 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771099 68370 0 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
51030054 84194 0 None -23 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086684 84194 0 None -23 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
51030054 84194 0 None -23 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086684 84194 0 None -23 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
68230018 129069 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598096 129069 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 459 7 0 8 2.5 C[C@H](CF)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
145993236 173572 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 591 6 1 6 6.3 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccc(C(=O)O)cc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4284231 173572 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 591 6 1 6 6.3 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccc(C(=O)O)cc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
54580880 7800 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 O=C(N1CCC(CC1)C1CCN(CC1)c1cccnc1)OC(C)(C)C 10.1016/j.bmcl.2010.12.086
5745 7800 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 O=C(N1CCC(CC1)C1CCN(CC1)c1cccnc1)OC(C)(C)C 10.1016/j.bmcl.2010.12.086
CHEMBL1770918 7800 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 O=C(N1CCC(CC1)C1CCN(CC1)c1cccnc1)OC(C)(C)C 10.1016/j.bmcl.2010.12.086
54591792 157332 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.4 O=C1NN=C(c2ccc3nc(-c4ccccc4)oc3c2)C2CCC12 nan
CHEMBL3954848 157332 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 317 2 1 4 3.4 O=C1NN=C(c2ccc3nc(-c4ccccc4)oc3c2)C2CCC12 nan
71081517 173673 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 471 3 0 5 5.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(C)(=O)=O)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4286139 173673 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 471 3 0 5 5.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(C)(=O)=O)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
68021765 164250 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 472 5 1 7 3.7 CCNC(=O)c1cc(F)c(-c2cc3nnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
CHEMBL4079321 164250 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 472 5 1 7 3.7 CCNC(=O)c1cc(F)c(-c2cc3nnn(C4CCN(C(=O)OC(C)C)CC4)c3cn2)cc1F 10.1016/j.bmc.2017.06.014
76309731 110002 0 None 204 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084368 110002 0 None 204 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC2CC2)c1C 10.1016/j.bmcl.2011.04.035
67464752 149590 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 405 6 1 5 5.2 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)[C@H]1C nan
CHEMBL3892950 149590 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 405 6 1 5 5.2 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)[C@H]1C nan
54592034 152653 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C(C)C)C(C)C)cc3)oc2c1 nan
CHEMBL3917552 152653 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C(C)C)C(C)C)cc3)oc2c1 nan
118711788 120815 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 474 6 0 8 2.5 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326680 120815 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 474 6 0 8 2.5 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
67464658 150667 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 298 2 1 5 2.4 O=C1CCC(c2ccc3nc(N4CCCCC4)oc3c2)=NN1 nan
CHEMBL3901874 150667 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 298 2 1 5 2.4 O=C1CCC(c2ccc3nc(N4CCCCC4)oc3c2)=NN1 nan
54586777 68348 0 None -3 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771076 68348 0 None -3 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
86689070 160068 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 425 3 1 7 3.2 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N4CCOCC4)nc3Cl)oc2c1 nan
CHEMBL3977848 160068 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 425 3 1 7 3.2 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N4CCOCC4)nc3Cl)oc2c1 nan
71720493 93753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 7 0 7 4.7 CC(C)c1noc(N2CCC(CO[C@H]3CC[C@H](c4ccc(S(C)(=O)=O)cc4F)CC3)CC2)n1 10.1021/ml300399u
CHEMBL2323593 93753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 7 0 7 4.7 CC(C)c1noc(N2CCC(CO[C@H]3CC[C@H](c4ccc(S(C)(=O)=O)cc4F)CC3)CC2)n1 10.1021/ml300399u
66554760 93761 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 397 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(COC2CC=C(c3ccncc3C#N)CC2)CC1 10.1021/ml300399u
CHEMBL2323601 93761 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 397 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(COC2CC=C(c3ccncc3C#N)CC2)CC1 10.1021/ml300399u
54583896 68368 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771097 68368 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
76327868 110003 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 438 6 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084369 110003 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 438 6 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
76324302 110024 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 428 6 0 7 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084392 110024 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 428 6 0 7 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
118720406 122293 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 465 5 0 5 5.4 CCOC(=O)[C@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3352841 122293 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 465 5 0 5 5.4 CCOC(=O)[C@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
122184143 129079 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 519 6 0 7 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598105 129079 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 519 6 0 7 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)C4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
71654940 97537 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 397 5 1 5 4.3 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(F)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391607 97537 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 397 5 1 5 4.3 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(F)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
71655014 97540 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 463 6 1 6 5.1 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391610 97540 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 463 6 1 6 5.1 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
72945896 111396 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 498 6 2 6 4.9 Cc1cc2c(c(Nc3ccc(C)c(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104885 111396 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 498 6 2 6 4.9 Cc1cc2c(c(Nc3ccc(C)c(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
54590846 160397 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 421 5 1 4 5.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(/C=C/c4ccccc4)cc3)oc2c1 nan
CHEMBL3980791 160397 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 421 5 1 4 5.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(/C=C/c4ccccc4)cc3)oc2c1 nan
67464896 167248 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 391 5 1 5 4.8 CC[C@@H]1C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)=NNC(=O)[C@@H]1C nan
CHEMBL4111799 167248 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 391 5 1 5 4.8 CC[C@@H]1C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)=NNC(=O)[C@@H]1C nan
71287378 117664 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 512 8 0 6 4.6 CCCc1cnc(N2CCC(C3Cc4cc(C5CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261133 117664 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 512 8 0 6 4.6 CCCc1cnc(N2CCC(C3Cc4cc(C5CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
118722584 122946 0 None 2 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 6 0 10 3.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(N=S(C)(C)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358009 122946 0 None 2 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 6 0 10 3.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(N=S(C)(C)=O)cc2F)cn1 10.1021/jm5011012
54583893 68355 0 None 17 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 399 4 0 5 3.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771083 68355 0 None 17 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 399 4 0 5 3.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
68299301 120325 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 502 4 0 8 4.6 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3)csc12)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321826 120325 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 502 4 0 8 4.6 CN(c1ncnc2c(-c3ccc(S(C)(=O)=O)cc3)csc12)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2014.07.020
137641046 163774 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 524 6 1 8 4.5 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1C(F)(F)F 10.1016/j.bmc.2017.06.014
CHEMBL4073169 163774 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 524 6 1 8 4.5 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)cc1C(F)(F)F 10.1016/j.bmc.2017.06.014
155569398 182923 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 4 0 7 4.3 CN(c1ncnc2c1CCN2c1ccc(S(C)(=O)=O)cc1F)[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4592464 182923 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 4 0 7 4.3 CN(c1ncnc2c1CCN2c1ccc(S(C)(=O)=O)cc1F)[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
71546856 93019 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 488 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312516 93019 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 488 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
58190389 84177 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 C[C@H]1CN(C(=O)OC(C)(C)C)[C@H](C)CN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086665 84177 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 C[C@H]1CN(C(=O)OC(C)(C)C)[C@H](C)CN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
60155365 84182 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 409 4 0 7 3.4 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(C#N)cc2)cn1 10.1021/jm300310c
CHEMBL2086670 84182 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 409 4 0 7 3.4 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(C#N)cc2)cn1 10.1021/jm300310c
66963587 117544 0 None -4 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 454 6 0 6 4.9 CCOC(=O)[C@](C)(Cc1ccccc1)c1cnnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260540 117544 0 None -4 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 454 6 0 6 4.9 CCOC(=O)[C@](C)(Cc1ccccc1)c1cnnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
89995716 154586 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 463 5 1 4 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C(N)=O)cc3)cc2)C2CC2)CC1 nan
CHEMBL3932795 154586 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 463 5 1 4 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C(N)=O)cc3)cc2)C2CC2)CC1 nan
67464536 166696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 4 1 4 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@@H]1C nan
CHEMBL4107094 166696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 4 1 4 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@@H]1C nan
44177589 89839 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 506 5 0 8 3.7 CC(C)(C)COC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181695 89839 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 506 5 0 8 3.7 CC(C)(C)COC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
51030054 84194 0 None -23 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL2086684 84194 0 None -23 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
137645678 164791 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 492 4 1 10 3.2 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncc(O)cn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
CHEMBL4085517 164791 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 492 4 1 10 3.2 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncc(O)cn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
54591107 156775 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 308 1 1 5 1.8 O=C1NN=C(N2CCc3nc(-c4ccccc4)oc3C2)C2CC12 nan
CHEMBL3950174 156775 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 308 1 1 5 1.8 O=C1NN=C(N2CCc3nc(-c4ccccc4)oc3C2)C2CC12 nan
67464830 154384 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 6 2 6 3.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)O)cc3)oc2c1 nan
CHEMBL3931151 154384 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 6 2 6 3.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(=O)O)cc3)oc2c1 nan
89995546 156588 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 485 5 1 7 4.2 CC(=O)Nc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)s1 nan
CHEMBL3948646 156588 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 485 5 1 7 4.2 CC(=O)Nc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)s1 nan
67466888 152808 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 6 2 6 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)O)cc3)oc2c1 nan
CHEMBL3918724 152808 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 393 6 2 6 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)O)cc3)oc2c1 nan
70693585 79837 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 451 6 0 8 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2nc3c(s2)CCCC3)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010843 79837 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 451 6 0 8 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2nc3c(s2)CCCC3)CC1 10.1016/j.bmcl.2011.10.033
67463367 156175 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 292 2 2 4 2.5 O=C1NCC(c2ccc3nc(-c4ccccc4)oc3c2)=NN1 nan
CHEMBL3945579 156175 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 292 2 2 4 2.5 O=C1NCC(c2ccc3nc(-c4ccccc4)oc3c2)=NN1 nan
54590931 156302 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(F)c(OC)c3)oc2c1 nan
CHEMBL3946528 156302 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 3.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(F)c(OC)c3)oc2c1 nan
67462495 156462 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)(C)N4CCCC4)cc3)oc2c1 nan
CHEMBL3947616 156462 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)(C)N4CCCC4)cc3)oc2c1 nan
24899996 89299 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 499 6 0 8 1.4 CN(C)S(=O)(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177766 89299 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 499 6 0 8 1.4 CN(C)S(=O)(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
58017059 89831 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 425 4 0 7 3.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(C#N)c(F)c2)CC1 10.1021/jm301404a
CHEMBL2181686 89831 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 425 4 0 7 3.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(C#N)c(F)c2)CC1 10.1021/jm301404a
71459321 89834 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 446 5 0 7 4.4 CSc1ccc(N2CCc3c(OC4CCN(C(=O)OC(C)C)CC4)ncnc32)cc1F 10.1021/jm301404a
CHEMBL2181689 89834 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 446 5 0 7 4.4 CSc1ccc(N2CCc3c(OC4CCN(C(=O)OC(C)C)CC4)ncnc32)cc1F 10.1021/jm301404a
90665949 116059 0 None -15 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3218816 116059 0 None -15 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
162648980 186628 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 548 8 1 12 0.4 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(CC)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4745258 186628 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 548 8 1 12 0.4 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(CC)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
67461007 151319 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 330 2 1 5 3.2 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C#N)cc3)oc2c1 nan
CHEMBL3907277 151319 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 330 2 1 5 3.2 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C#N)cc3)oc2c1 nan
168273301 197314 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 480 5 0 8 3.8 CCc1cnc(N2CCC(n3ncc4ccc(-c5ccc(S(C)(=O)=O)cc5F)nc43)CC2)cn1 10.1016/j.bmc.2022.116614
CHEMBL5179691 197314 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 480 5 0 8 3.8 CCc1cnc(N2CCC(n3ncc4ccc(-c5ccc(S(C)(=O)=O)cc5F)nc43)CC2)cn1 10.1016/j.bmc.2022.116614
53235534 7905 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 10.1016/j.bmcl.2010.12.086
5748 7905 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 10.1016/j.bmcl.2010.12.086
CHEMBL1771100 7905 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 10.1016/j.bmcl.2010.12.086
44467185 68371 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 7 0 7 4.0 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cc3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771101 68371 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 7 0 7 4.0 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cc3)CC2)nc1 10.1016/j.bmcl.2010.12.086
127050519 147791 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 480 5 0 8 3.8 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
CHEMBL3823780 147791 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 480 5 0 8 3.8 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc43)CC2)nc1 10.1016/j.bmcl.2016.06.050
68039954 130777 0 None 8 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 5 1 8 4.1 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629484 130777 0 None 8 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 5 1 8 4.1 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
145977018 170342 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 401 8 0 3 5.7 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CC2)CC(C)(C)CO3)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4203148 170342 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 401 8 0 3 5.7 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CC2)CC(C)(C)CO3)cc1 10.1016/j.bmcl.2018.02.044
145976125 170541 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 401 8 0 3 5.7 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CC2)COC(C)(C)C3)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4205617 170541 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 401 8 0 3 5.7 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CC2)COC(C)(C)C3)cc1 10.1016/j.bmcl.2018.02.044
118722578 122939 0 None 10 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 532 7 0 11 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358002 122939 0 None 10 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 532 7 0 11 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
118722581 122942 0 None 7 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358005 122942 0 None 7 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 516 6 0 10 2.7 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
118722585 122948 0 None 7 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 564 7 0 10 2.5 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358011 122948 0 None 7 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 564 7 0 10 2.5 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
66963996 117539 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 449 8 0 6 4.7 COCCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260535 117539 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 449 8 0 6 4.7 COCCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
73350444 96972 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 422 4 0 8 2.9 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1016/j.bmcl.2013.04.006
CHEMBL2382410 96972 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 422 4 0 8 2.9 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1016/j.bmcl.2013.04.006
53469852 79846 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 486 6 0 4 3.7 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010851 79846 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 486 6 0 4 3.7 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
53235534 7905 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 10.1016/j.bmcl.2010.12.086
5748 7905 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 10.1016/j.bmcl.2010.12.086
CHEMBL1771100 7905 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 10.1016/j.bmcl.2010.12.086
44467183 68372 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 425 7 0 8 3.4 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cn3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771102 68372 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 425 7 0 8 3.4 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cn3)CC2)nc1 10.1016/j.bmcl.2010.12.086
11271424 68868 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 6 0 9 2.9 CC(C)COC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775173 68868 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 6 0 9 2.9 CC(C)COC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
90115611 130509 0 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 451 8 0 7 3.8 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
CHEMBL3622167 130509 0 None 2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 451 8 0 7 3.8 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
90148901 130513 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 449 8 0 7 3.1 COc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622170 130513 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 449 8 0 7 3.1 COc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
86717800 130523 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 481 9 0 7 3.4 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3cc(F)c(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622180 130523 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 481 9 0 7 3.4 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3cc(F)c(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
122191631 130516 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 437 7 0 6 3.2 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(F)cn3)CC2)cc1F 10.1021/acsmedchemlett.5b00207
CHEMBL3622173 130516 0 None -1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 437 7 0 6 3.2 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(F)cn3)CC2)cc1F 10.1021/acsmedchemlett.5b00207
71128816 130519 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622176 130519 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
164624288 192809 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4870635 192809 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
25053185 183656 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 515 9 1 11 4.2 CCCS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL461558 183656 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 515 9 1 11 4.2 CCCS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
118711797 120823 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 516 7 0 10 2.6 CCc1cnc(C(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)nc1 10.1016/j.bmcl.2014.06.071
CHEMBL3326688 120823 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 516 7 0 10 2.6 CCc1cnc(C(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)nc1 10.1016/j.bmcl.2014.06.071
53492264 129074 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598100 129074 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
71116111 130511 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 429 7 0 7 3.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)CC1 10.1021/acsmedchemlett.5b00207
CHEMBL3622169 130511 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 429 7 0 7 3.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)CC1 10.1021/acsmedchemlett.5b00207
71136686 130510 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 441 8 0 9 3.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
CHEMBL3622168 130510 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 441 8 0 9 3.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(-n4cnnn4)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
164624288 192809 0 None -1 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR119 in golden hamster HIT-T15 cells assessed as induction of glucose-induced insulin secretion after 2 hrs by A1phaLISAAgonist activity at rat GPR119 in golden hamster HIT-T15 cells assessed as induction of glucose-induced insulin secretion after 2 hrs by A1phaLISA
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
CHEMBL4870635 192809 0 None -1 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR119 in golden hamster HIT-T15 cells assessed as induction of glucose-induced insulin secretion after 2 hrs by A1phaLISAAgonist activity at rat GPR119 in golden hamster HIT-T15 cells assessed as induction of glucose-induced insulin secretion after 2 hrs by A1phaLISA
ChEMBL 551 7 0 10 2.9 CC(C)(F)c1noc(N2CCC(N(c3cc(OC4CCN(S(C)(=O)=O)CC4)ncn3)C(F)(F)F)CC2)n1 10.1016/j.bmc.2021.116208
118711781 120808 0 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 498 5 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326673 120808 0 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 498 5 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
156020541 184929 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 446 7 0 10 3.3 CCc1cnc(N2CC=C(c3nc(COc4ccc(-n5cnnn5)cc4)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
CHEMBL4648870 184929 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 446 7 0 10 3.3 CCc1cnc(N2CC=C(c3nc(COc4ccc(-n5cnnn5)cc4)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
137631845 163062 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 522 6 2 10 3.5 CC(C)(C)OC(=O)N1CC2CC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4065265 163062 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 522 6 2 10 3.5 CC(C)(C)OC(=O)N1CC2CC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
71562845 110053 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 519 6 1 10 3.8 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084480 110053 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 519 6 1 10 3.8 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Nc3ccc(S(C)(=O)=O)cc3)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
140251527 171839 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 462 7 1 5 3.8 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N3CC(O)C3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4226586 171839 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 462 7 1 5 3.8 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N3CC(O)C3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
11224944 68866 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 459 5 0 9 2.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2013.12.127
CHEMBL1775171 68866 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 459 5 0 9 2.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2013.12.127
76317600 111698 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 560 6 0 7 6.4 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(F)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112990 111698 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 560 6 0 7 6.4 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(F)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
71545698 93020 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 518 4 0 8 4.2 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312517 93020 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 518 4 0 8 4.2 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71545381 93028 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 3 0 7 4.4 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)(C)C)c1C 10.1021/jm301626p
CHEMBL2312524 93028 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 3 0 7 4.4 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)(C)C)c1C 10.1021/jm301626p
66964599 117528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 433 6 0 5 5.4 CCOC(=O)C(C)(Cc1cccc(C)c1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260522 117528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 433 6 0 5 5.4 CCOC(=O)C(C)(Cc1cccc(C)c1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
66964466 117533 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 426 6 0 7 4.6 CCOC(=O)C(C)(Cc1cscn1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260527 117533 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 426 6 0 7 4.6 CCOC(=O)C(C)(Cc1cscn1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
11271133 68609 0 None -2 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 460 5 0 9 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)noc23)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773294 68609 0 None -2 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 460 5 0 9 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)noc23)CC1 10.1016/j.bmcl.2011.03.007
118711797 120823 0 None -8 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 516 7 0 10 2.6 CCc1cnc(C(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)nc1 10.1016/j.bmcl.2014.06.071
CHEMBL3326688 120823 0 None -8 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 516 7 0 10 2.6 CCc1cnc(C(=O)N2CCC(Oc3ncnc(Oc4ccc(S(C)(=O)=O)nc4C)c3F)CC2)nc1 10.1016/j.bmcl.2014.06.071
25053040 179891 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 438 7 1 11 2.5 CCOC(=O)C1CCN(c2ncnc(Nc3ccc(-n4cncn4)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL452056 179891 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayAgonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 438 7 1 11 2.5 CCOC(=O)C1CCN(c2ncnc(Nc3ccc(-n4cncn4)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
53492593 129062 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 461 5 0 6 4.2 Cc1nc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)ccc1C(=O)N(C)C 10.1016/j.bmcl.2015.04.102
CHEMBL3598089 129062 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 461 5 0 6 4.2 Cc1nc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)ccc1C(=O)N(C)C 10.1016/j.bmcl.2015.04.102
71655095 97465 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 513 7 1 7 5.7 CCOC(=O)c1cc(C(C)(C)C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
CHEMBL2391431 97465 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 513 7 1 7 5.7 CCOC(=O)c1cc(C(C)(C)C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
118300922 153221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 450 5 0 4 5.4 COc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
CHEMBL3922037 153221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 450 5 0 4 5.4 COc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
89995524 157046 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 2 7 4.0 CNC(=O)Nc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)s1 nan
CHEMBL3952520 157046 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 2 7 4.0 CNC(=O)Nc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)s1 nan
162650857 187128 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 588 7 1 12 0.9 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(C(F)(F)F)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4751384 187128 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 588 7 1 12 0.9 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3ncc(C(F)(F)F)cn3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
54584625 68999 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 453 6 0 8 3.2 CC(C)OC(=O)N1CCC(Oc2cc(Oc3ccc(S(C)(=O)=O)cc3F)ncn2)CC1 10.1016/j.bmcl.2011.04.035
CHEMBL1778140 68999 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 453 6 0 8 3.2 CC(C)OC(=O)N1CCC(Oc2cc(Oc3ccc(S(C)(=O)=O)cc3F)ncn2)CC1 10.1016/j.bmcl.2011.04.035
118711792 120818 0 None -5 2 Rat 6.4 pEC50 = 6.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 6 0 8 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3CCCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326683 120818 0 None -5 2 Rat 6.4 pEC50 = 6.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 6 0 8 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3CCCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
53325083 65338 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 386 6 1 3 3.4 CC(C)OC(=O)N1CCC(CCNC(=O)Cc2c(F)ccc(F)c2F)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684039 65338 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 386 6 1 3 3.4 CC(C)OC(=O)N1CCC(CCNC(=O)Cc2c(F)ccc(F)c2F)CC1 10.1016/j.bmcl.2011.01.088
86694584 140573 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 473 4 0 7 3.7 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(c5ncc(Cl)cn5)CC4)oc3cn2)CC1 nan
CHEMBL3715366 140573 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 473 4 0 7 3.7 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(c5ncc(Cl)cn5)CC4)oc3cn2)CC1 nan
56592327 165570 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 504 5 0 9 4.1 CCc1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
CHEMBL4094202 165570 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 504 5 0 9 4.1 CCc1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
11224944 68866 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 459 5 0 9 2.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2013.11.053
CHEMBL1775171 68866 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 459 5 0 9 2.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2013.11.053
58190405 84171 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086659 84171 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
54581961 68362 0 None 1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 4 0 6 3.5 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C#N)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771091 68362 0 None 1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 4 0 6 3.5 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C#N)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
51029601 84164 3 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086650 84164 3 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
51029601 84164 3 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086650 84164 3 None -1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
89995526 151544 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 421 4 0 4 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3)cc2)C2CC2)CC1 nan
CHEMBL3909108 151544 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 421 4 0 4 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3)cc2)C2CC2)CC1 nan
54590847 167130 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 3.7 CC[C@H]1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL4110815 167130 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 3.7 CC[C@H]1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
67465964 167286 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 362 4 1 5 3.8 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(N(C)C)cc3)oc2c1 nan
CHEMBL4112167 167286 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 362 4 1 5 3.8 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(N(C)C)cc3)oc2c1 nan
118711780 120807 0 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326672 120807 0 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
67464498 152305 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 289 2 1 4 3.2 O=c1ccc(-c2ccc3nc(-c4ccccc4)oc3c2)n[nH]1 nan
CHEMBL3914956 152305 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 289 2 1 4 3.2 O=c1ccc(-c2ccc3nc(-c4ccccc4)oc3c2)n[nH]1 nan
67464934 150088 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 4 4.0 CC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3Cl)oc2c1 nan
CHEMBL3897150 150088 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 4 4.0 CC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3Cl)oc2c1 nan
67467264 166979 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@@H]2CCc3nc(-c4ccccc4)oc3C2)[C@H]2C[C@@H]12 nan
CHEMBL4109527 166979 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@@H]2CCc3nc(-c4ccccc4)oc3C2)[C@H]2C[C@@H]12 nan
67466276 152376 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 429 6 1 7 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cncn4C)cc3)oc2c1 nan
CHEMBL3915473 152376 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 429 6 1 7 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cncn4C)cc3)oc2c1 nan
66556985 93756 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 512 6 0 7 4.6 Cc1nc(S(C)(=O)=O)ccc1[C@H]1CC[C@H](OCC2CCN(c3ncc(C(F)(F)F)cn3)CC2)CC1 10.1021/ml300399u
CHEMBL2323596 93756 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 512 6 0 7 4.6 Cc1nc(S(C)(=O)=O)ccc1[C@H]1CC[C@H](OCC2CCN(c3ncc(C(F)(F)F)cn3)CC2)CC1 10.1021/ml300399u
54586012 68610 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 467 5 0 10 3.1 CC(C)c1noc(C2CCN(c3ncnc4c3cnn4-c3ccc(S(C)(=O)=O)cc3)CC2)n1 10.1016/j.bmcl.2011.03.007
CHEMBL1773295 68610 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 467 5 0 10 3.1 CC(C)c1noc(C2CCN(c3ncnc4c3cnn4-c3ccc(S(C)(=O)=O)cc3)CC2)n1 10.1016/j.bmcl.2011.03.007
56592328 166283 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 510 4 0 9 4.1 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncc(Cl)cn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
CHEMBL4101938 166283 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 510 4 0 9 4.1 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncc(Cl)cn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
68022224 147696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 442 4 0 7 3.7 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3822500 147696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 442 4 0 7 3.7 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmcl.2016.06.050
68022224 147696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 442 4 0 7 3.7 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmc.2017.06.014
CHEMBL3822500 147696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 442 4 0 7 3.7 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc32)CC1 10.1016/j.bmc.2017.06.014
155532730 178539 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 477 6 1 7 4.8 CCc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4467458 178539 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 477 6 1 7 4.8 CCc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
76324300 110012 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 484 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(F)cc2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084379 110012 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 484 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)c2ccc(F)cc2)c1C 10.1016/j.bmcl.2011.04.035
145949313 169673 0 None -8 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 485 5 1 7 5.3 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CCC1 10.1021/acsmedchemlett.8b00073
CHEMBL4173664 169673 0 None -8 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 485 5 1 7 5.3 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CCC1 10.1021/acsmedchemlett.8b00073
118722578 122939 0 None -10 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 532 7 0 11 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358002 122939 0 None -10 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 532 7 0 11 2.7 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(OS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
11190983 68605 0 None -2 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 487 4 0 9 3.3 Cc1nn(-c2ccc(S(C)(=O)=O)cc2)c2ncnc(OC3CCN(C(=O)OC(C)(C)C)CC3)c12 10.1016/j.bmcl.2011.03.007
CHEMBL1773288 68605 0 None -2 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 487 4 0 9 3.3 Cc1nn(-c2ccc(S(C)(=O)=O)cc2)c2ncnc(OC3CCN(C(=O)OC(C)(C)C)CC3)c12 10.1016/j.bmcl.2011.03.007
11465648 68608 0 None -5 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 474 4 0 10 2.4 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2nnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773291 68608 0 None -5 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 474 4 0 10 2.4 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2nnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
68209225 161160 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 362 4 1 5 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N(C)C)cc3)oc2c1 nan
CHEMBL3987172 161160 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 362 4 1 5 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(N(C)C)cc3)oc2c1 nan
118300912 167004 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 433 5 0 6 3.0 CC(C)OC(=O)N1CC[C@H](N(C(=O)c2ccc(-n3cncn3)c(F)c2)C2CC2)[C@H](F)C1 nan
CHEMBL4109770 167004 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).LANCE cAMP Assay: Quantitative detection of cAMP accumulation from cells expressing human GPR119 receptor is achieved using Perkin Elmer's LANCE cAMP-384 Kit (Cat#AD0264) according to the manufacturer's protocol. Briefly, HEK293 cells stably expressing a mutant form of the human GPR119 receptor as assay tool (Methionine 1 replaced with the amino acid sequence MKTIIALSYIFCLVFADYKDDDDA, and T327 & S329 changed to alanines; SEQ ID No. 1) are grown to 50-70% confluency in cell culture media (DMEM, 10% heat inactivated Fetal Bovine Serum, 50 I.U./mL penicillin, 50 ug/mL streptomycin, 10 mM HEPES, 20 ug/mL G418 Sulfate). On the day of the assay, GPR119 stable HEK293 cells are lifted from the tissue culture plate and 1000 cells/well are incubated along with various concentrations of test compounds for 20 min at 37° C. Detection Buffer (50 mM HEPES, 10 mM calcium chloride, 0.35% Triton X-100, 1 mg/mL BSA) containing cAMP-specific antibody is then added to all wells and allowed to equilibrate in the dark for 10 minutes at room temperature. Upon equilibration, Detection Buffer containing europium-labeled cAMP tracer complex is added to all wells and allowed to react for 1 hour at room temperature. After 1 hour, bound europium-labeled cAMP tracer is measured using a Perkin Elmer Envision plate reader. The quantity of cAMP generated in each well is derived from a standard curve. EC50 is determined using nonlinear regression analysis of the cAMP values over a range of agonist concentration (12 points spanning the range from 30 uM to 100 pM).
ChEMBL 433 5 0 6 3.0 CC(C)OC(=O)N1CC[C@H](N(C(=O)c2ccc(-n3cncn3)c(F)c2)C2CC2)[C@H](F)C1 nan
11691484 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
5727 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
CHEMBL1951032 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
DB12084 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
11691484 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
5727 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
CHEMBL1951032 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
DB12084 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
11691484 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
5727 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
CHEMBL1951032 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
DB12084 8921 51 None -8 2 Rat 6.4 pEC50 = 6.4 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
73387819 157934 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 424 4 0 5 4.1 Cn1cc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
CHEMBL3959571 157934 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 424 4 0 5 4.1 Cn1cc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
54591184 155427 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(C(C)C)C(C)C)c3)oc2c1 nan
CHEMBL3939535 155427 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(C(C)C)C(C)C)c3)oc2c1 nan
155564944 182276 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 448 6 0 7 4.5 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)cc2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4577659 182276 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 448 6 0 7 4.5 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)cc2)no1 10.1016/j.bmcl.2019.07.004
68209164 160492 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccccn4)c3)oc2c1 nan
CHEMBL3981568 160492 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4ccccn4)c3)oc2c1 nan
67450901 129076 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 469 6 0 9 2.0 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC4CCOC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598102 129076 0 None 3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 469 6 0 9 2.0 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC4CCOC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
164627706 193224 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 522 5 1 8 3.0 CC(C)(C)OC(=O)N1CCC(N(c2cc(NC3CCN(S(C)(=O)=O)CC3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
CHEMBL4876465 193224 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 522 5 1 8 3.0 CC(C)(C)OC(=O)N1CCC(N(c2cc(NC3CCN(S(C)(=O)=O)CC3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
75202770 189116 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 512 5 1 9 4.7 Cc1c(Oc2cccc(/C=C3\SC(=O)NC3=O)c2)ncnc1OC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116071
CHEMBL4784457 189116 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 512 5 1 9 4.7 Cc1c(Oc2cccc(/C=C3\SC(=O)NC3=O)c2)ncnc1OC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116071
68036465 169295 0 None -7 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 485 6 1 8 3.8 CCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4167676 169295 0 None -7 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 485 6 1 8 3.8 CCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
68040038 130778 0 None -6 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 499 6 1 9 3.8 COc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629485 130778 0 None -6 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 499 6 1 9 3.8 COc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
118711796 120822 0 None 13 2 Human 7.4 pEC50 = 7.4 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3nc(C(C)(C)F)no3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326687 120822 0 None 13 2 Human 7.4 pEC50 = 7.4 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3nc(C(C)(C)F)no3)CC2)c1F 10.1016/j.bmcl.2014.06.071
58114293 90446 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
CHEMBL2204982 90446 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as cAMP level by beta-lactamase reporter gene assay
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
25053043 179765 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 487 8 1 11 3.3 CCCc1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL451794 179765 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 487 8 1 11 3.3 CCCc1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
155566096 182524 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 C[C@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4583270 182524 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 C[C@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
76321324 111711 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 556 6 0 7 6.6 O=S(=O)(c1ccc(Cl)cc1)N1CCCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113003 111711 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 556 6 0 7 6.6 O=S(=O)(c1ccc(Cl)cc1)N1CCCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
54591570 155314 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 514 7 1 6 6.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC5(CCCCC5)CC4)cc3)oc2c1 nan
CHEMBL3938622 155314 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 514 7 1 6 6.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC5(CCCCC5)CC4)cc3)oc2c1 nan
21897616 68870 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 5 0 10 2.0 CS(=O)(=O)c1ccc(-n2ncc3c(OC4CCN(C(=O)OC5CCOC5)CC4)ncnc32)cc1 10.1016/j.bmcl.2011.03.007
CHEMBL1775175 68870 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 5 0 10 2.0 CS(=O)(=O)c1ccc(-n2ncc3c(OC4CCN(C(=O)OC5CCOC5)CC4)ncnc32)cc1 10.1016/j.bmcl.2011.03.007
118720424 122680 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 426 3 1 4 5.1 CC1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354796 122680 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 426 3 1 4 5.1 CC1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
90665949 116059 0 None -15 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm5011012
CHEMBL3218816 116059 0 None -15 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm5011012
67466081 150878 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 434 8 1 6 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C)C(C)C)cc3)oc2c1 nan
CHEMBL3903547 150878 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 434 8 1 6 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C)C(C)C)cc3)oc2c1 nan
70687121 84578 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 412 6 1 3 3.8 C[C@H](CNC(=O)Cc1c(F)ccc(F)c1F)C1CCN(C(=O)OC2(C)CC2)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL2092727 84578 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 412 6 1 3 3.8 C[C@H](CNC(=O)Cc1c(F)ccc(F)c1F)C1CCN(C(=O)OC2(C)CC2)CC1 10.1016/j.bmcl.2011.01.088
145983474 172357 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 525 5 2 10 3.9 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4242383 172357 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 525 5 2 10 3.9 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4)ncnc13)C2 10.1016/j.bmc.2018.06.035
122194338 130772 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 538 5 1 9 4.1 Cc1c(Nc2ccc(S(C)(=O)=O)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
CHEMBL3629479 130772 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 538 5 1 9 4.1 Cc1c(Nc2ccc(S(C)(=O)=O)cc2Cl)ncnc1OC1CC2COCC(C1)N2C(=O)OC(C)(C)C 10.1016/j.bmcl.2015.09.047
76309733 110015 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 449 6 0 6 4.1 Cc1c(Oc2ccccc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084382 110015 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 449 6 0 6 4.1 Cc1c(Oc2ccccc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
11663249 77618 0 None 11 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 493 8 1 10 3.1 CCOc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951033 77618 0 None 11 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 493 8 1 10 3.1 CCOc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
76317689 111848 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 3.9 Cc1cc(S(C)(=O)=O)cc2c1N(C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1)CC2 10.1016/j.bmc.2014.01.028
CHEMBL3113835 111848 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 3.9 Cc1cc(S(C)(=O)=O)cc2c1N(C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1)CC2 10.1016/j.bmc.2014.01.028
46939910 169839 0 None -2 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(F)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4176348 169839 0 None -2 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 464 5 1 7 3.7 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(F)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
58190347 84174 0 None 1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CCN1C(=O)OC(C)(C)C 10.1021/jm300310c
CHEMBL2086662 84174 0 None 1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CCN1C(=O)OC(C)(C)C 10.1021/jm300310c
155515010 176696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4441091 176696 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 466 6 0 7 4.6 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
89995618 150054 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 516 5 0 5 4.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3F)cc2)C2CC2)CC1 nan
CHEMBL3896881 150054 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 516 5 0 5 4.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3F)cc2)C2CC2)CC1 nan
134136992 149825 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 476 5 0 8 5.1 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Oc3ccccc3Cl)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3894993 149825 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 476 5 0 8 5.1 CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ncnc(Oc3ccccc3Cl)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
71655015 97541 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 409 6 1 6 4.2 COc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.04.014
CHEMBL2391611 97541 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 409 6 1 6 4.2 COc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.04.014
70680970 79835 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 472 7 0 9 2.7 Cc1nc(-c2ccc(CN3CCC(N(C)C(=O)Cc4ccc(-n5cnnn5)cc4)CC3)cc2)no1 10.1016/j.bmcl.2011.10.033
CHEMBL2010841 79835 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 472 7 0 9 2.7 Cc1nc(-c2ccc(CN3CCC(N(C)C(=O)Cc4ccc(-n5cnnn5)cc4)CC3)cc2)no1 10.1016/j.bmcl.2011.10.033
54590933 160590 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OC(C)C)c3)oc2c1 nan
CHEMBL3982393 160590 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OC(C)C)c3)oc2c1 nan
67466128 166941 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 2.7 CO[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL4109212 166941 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 2.7 CO[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
73387820 154480 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 427 6 1 6 3.3 CC(C)(O)COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3931982 154480 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 427 6 1 6 3.3 CC(C)(O)COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
71736416 140499 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 449 4 1 5 5.4 CCNC(=O)c1ccc(-c2cc3cc(C4CCN(C(=O)OC(C)(C)C)CC4)oc3cn2)cc1 nan
CHEMBL3715068 140499 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 449 4 1 5 5.4 CCNC(=O)c1ccc(-c2cc3cc(C4CCN(C(=O)OC(C)(C)C)CC4)oc3cn2)cc1 nan
71713968 111398 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 509 7 1 6 5.0 O=C1c2cc(C3CC3)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2C(=O)N1C1CC1 10.1016/j.bmcl.2013.11.053
CHEMBL3104887 111398 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 509 7 1 6 5.0 O=C1c2cc(C3CC3)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2C(=O)N1C1CC1 10.1016/j.bmcl.2013.11.053
155567012 182641 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 476 5 1 7 4.6 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1N(C)[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4585818 182641 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 476 5 1 7 4.6 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1N(C)[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
51029964 84186 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 463 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cn2)cn1 10.1021/jm300310c
CHEMBL2086674 84186 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 463 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cn2)cn1 10.1021/jm300310c
54583894 68358 0 None 1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 4 0 6 3.3 Cc1cnc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771086 68358 0 None 1 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 4 0 6 3.3 Cc1cnc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
73351961 96979 0 None -11 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382417 96979 0 None -11 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
53491642 129058 0 None 1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 400 4 0 5 4.7 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(C#N)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598085 129058 0 None 1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 400 4 0 5 4.7 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(C#N)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
89995565 156805 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 6 0 5 4.2 CC(C)COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3950435 156805 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 6 0 5 4.2 CC(C)COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
89995521 157531 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2F)C2CC2)CC1 nan
CHEMBL3956393 157531 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2F)C2CC2)CC1 nan
89995723 158785 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 5 0 5 4.6 CC(C)(C)COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3966876 158785 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 5 0 5 4.6 CC(C)(C)COC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
71655250 97525 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 477 7 2 5 4.9 O=C(NC1CC1)c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391595 97525 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 477 7 2 5 4.9 O=C(NC1CC1)c1cc(Cl)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
145984093 172614 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 543 5 2 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4248698 172614 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 543 5 2 10 4.0 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@@H](Nc1ncnc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
54591020 160498 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 306 2 1 5 2.8 CC1CC(=O)NN=C1c1ccc2nc(-c3cccnc3)oc2c1 nan
CHEMBL3981614 160498 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 306 2 1 5 2.8 CC1CC(=O)NN=C1c1ccc2nc(-c3cccnc3)oc2c1 nan
70691486 79826 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 468 6 0 4 3.8 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010831 79826 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 468 6 0 4 3.8 CN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
67465258 157426 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 295 2 1 5 3.3 O=c1ccc(-c2ccc3nc(-c4cccs4)oc3c2)n[nH]1 nan
CHEMBL3955514 157426 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 295 2 1 5 3.3 O=c1ccc(-c2ccc3nc(-c4cccs4)oc3c2)n[nH]1 nan
51030336 84195 0 None -4 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 5 0 8 2.4 CC(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)[C@H](C)C1 10.1021/jm300310c
CHEMBL2086685 84195 0 None -4 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 396 5 0 8 2.4 CC(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)[C@H](C)C1 10.1021/jm300310c
139437037 182073 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 468 7 1 9 1.3 NC(=O)OC1CN(c2ncc(N3CC[C@@H](Oc4ccc(OCC(F)(F)F)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
CHEMBL4573031 182073 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 468 7 1 9 1.3 NC(=O)OC1CN(c2ncc(N3CC[C@@H](Oc4ccc(OCC(F)(F)F)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
11691484 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
5727 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
CHEMBL1951032 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
DB12084 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2015.04.102
71081450 174156 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 548 5 0 6 6.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4294852 174156 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 548 5 0 6 6.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
127048491 147761 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 471 4 0 6 4.3 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4cc(F)c(C(=O)N(C)C)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823379 147761 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 471 4 0 6 4.3 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4cc(F)c(C(=O)N(C)C)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
11691484 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
5727 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
CHEMBL1951032 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
DB12084 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2011.12.092
62706518 83015 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CC3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058403 83015 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CC3)CC1 10.1016/j.bmcl.2012.05.117
145963524 169101 0 None -5 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 459 5 1 7 4.8 CC(C)OC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
CHEMBL4164666 169101 0 None -5 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 459 5 1 7 4.8 CC(C)OC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
54591487 154614 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 504 8 1 7 4.9 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN5C[C@H](C)O[C@H](C)C5)cc4)oc3c2)[C@H]1C nan
CHEMBL3932982 154614 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 504 8 1 7 4.9 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN5C[C@H](C)O[C@H](C)C5)cc4)oc3c2)[C@H]1C nan
11691484 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
5727 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
CHEMBL1951032 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
DB12084 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 10.1016/j.bmcl.2014.06.071
67466262 157646 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 379 5 1 6 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)c(OC)c3)oc2c1 nan
CHEMBL3957279 157646 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 379 5 1 6 3.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)c(OC)c3)oc2c1 nan
89995556 151153 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 437 4 1 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(O)nc3)cc2)C2CC2)CC1 nan
CHEMBL3905812 151153 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 437 4 1 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(O)nc3)cc2)C2CC2)CC1 nan
71519027 93116 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 450 6 1 7 3.4 CS(=O)(=O)c1ccc(NCc2cnn(C3CCN(C(=O)OC4CCC4)CC3)c2)c(F)c1 10.1016/j.bmcl.2012.10.119
CHEMBL2313408 93116 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 450 6 1 7 3.4 CS(=O)(=O)c1ccc(NCc2cnn(C3CCN(C(=O)OC4CCC4)CC3)c2)c(F)c1 10.1016/j.bmcl.2012.10.119
67462519 149675 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 361 4 1 4 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C(C)C)cc3)oc2c1 nan
CHEMBL3893671 149675 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 361 4 1 4 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(C(C)C)cc3)oc2c1 nan
51029877 84175 2 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)C(C)(C)C1 10.1021/jm300310c
CHEMBL2086663 84175 2 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)C(C)(C)C1 10.1021/jm300310c
53491780 129071 0 None -7 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 477 8 0 8 2.5 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(CF)CF)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598098 129071 0 None -7 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 477 8 0 8 2.5 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(CF)CF)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
89995649 149849 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 436 4 0 5 4.5 Cc1cncnc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3895217 149849 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 436 4 0 5 4.5 Cc1cncnc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
67462376 157328 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 2 1 4 3.5 O=C1NN=C(c2ccc3nc(-c4ccc(F)cc4)oc3c2)C2CCC12 nan
CHEMBL3954798 157328 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 2 1 4 3.5 O=C1NN=C(c2ccc3nc(-c4ccc(F)cc4)oc3c2)C2CCC12 nan
67449879 129059 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 454 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598086 129059 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 454 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
71135993 171895 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 429 8 1 5 4.2 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NC3CC3)nc1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4227426 171895 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 429 8 1 5 4.2 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NC3CC3)nc1)C2 10.1016/j.bmc.2018.02.032
71716738 93117 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 502 7 1 9 3.2 CCc1cnc(OC(=O)N2CCC(n3cc(CNc4ccc(S(C)(=O)=O)cc4F)cn3)CC2)nc1 10.1016/j.bmcl.2012.10.119
CHEMBL2313409 93117 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 502 7 1 9 3.2 CCc1cnc(OC(=O)N2CCC(n3cc(CNc4ccc(S(C)(=O)=O)cc4F)cn3)CC2)nc1 10.1016/j.bmcl.2012.10.119
51030985 96976 0 None 64 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382414 96976 0 None 64 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
57392504 77616 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 499 7 1 9 3.7 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C(F)F 10.1016/j.bmcl.2011.12.092
CHEMBL1951030 77616 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 499 7 1 9 3.7 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C(F)F 10.1016/j.bmcl.2011.12.092
122194420 130792 0 None -9 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 6 1 9 3.3 COc1c(Nc2ccc(C#N)cc2F)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629597 130792 0 None -9 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 6 1 9 3.3 COc1c(Nc2ccc(C#N)cc2F)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
67464421 152762 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 6 1 7 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)oc2c1 nan
CHEMBL3918355 152762 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 6 1 7 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@@H]4CCCN4C(=O)OC(C)(C)C)cc3)oc2c1 nan
118711213 120708 0 None -7 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 536 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325846 120708 0 None -7 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 536 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
57401105 77601 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1nc(Nc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)ccc1S(C)(=O)=O 10.1016/j.bmcl.2011.12.092
CHEMBL1951014 77601 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1nc(Nc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)ccc1S(C)(=O)=O 10.1016/j.bmcl.2011.12.092
54580904 68359 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 433 4 0 5 4.3 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771088 68359 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 433 4 0 5 4.3 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
76683914 171896 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 463 9 2 5 3.2 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NCC(N)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4227435 171896 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 463 9 2 5 3.2 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NCC(N)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
118300933 150947 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 446 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cncc(C#N)c3)cc2)C2CC2)CC1 nan
CHEMBL3904060 150947 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 446 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cncc(C#N)c3)cc2)C2CC2)CC1 nan
137632674 163248 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 504 6 2 10 3.3 CC(C)(C)OC(=O)N1CC2CC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4067384 163248 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 504 6 2 10 3.3 CC(C)(C)OC(=O)N1CC2CC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
122184145 129084 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 505 7 0 7 4.2 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598110 129084 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 505 7 0 7 4.2 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
118711786 120813 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.2 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=S)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326678 120813 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.2 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=S)OC3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
76317666 111806 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 482 5 0 7 3.6 COc1cc2c(cc1S(C)(=O)=O)CCN2C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113635 111806 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 482 5 0 7 3.6 COc1cc2c(cc1S(C)(=O)=O)CCN2C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
70689387 79843 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 477 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)nc2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010849 79843 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 477 6 0 7 2.7 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)nc2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
60155097 84166 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
CHEMBL2086652 84166 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1021/jm300310c
11663249 77618 0 None -11 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 493 8 1 10 3.1 CCOc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951033 77618 0 None -11 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 493 8 1 10 3.1 CCOc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
67464351 152526 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 406 7 1 6 3.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C)C)cc3)oc2c1 nan
CHEMBL3916585 152526 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 406 7 1 6 3.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C)C)cc3)oc2c1 nan
70693582 79829 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 447 6 1 3 3.7 CNC(=O)c1ccc(CC(=O)N(C)C2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmcl.2011.10.033
CHEMBL2010834 79829 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 447 6 1 3 3.7 CNC(=O)c1ccc(CC(=O)N(C)C2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmcl.2011.10.033
145986139 172249 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 490 4 2 9 4.4 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1C[C@@H]2Nc1ncnc2c(Nc3ccc(C#N)cc3F)ncnc12 10.1016/j.bmc.2018.06.035
CHEMBL4239711 172249 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 490 4 2 9 4.4 CC(C)(C)OC(=O)N1C[C@@H]2CC[C@H]1C[C@@H]2Nc1ncnc2c(Nc3ccc(C#N)cc3F)ncnc12 10.1016/j.bmc.2018.06.035
145968709 171581 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 8 4.0 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)NC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4218430 171581 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 8 4.0 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)NC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
68036798 169220 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 501 7 1 9 3.0 COCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4166451 169220 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 501 7 1 9 3.0 COCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
71546035 93009 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 449 5 0 7 4.4 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312505 93009 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 449 5 0 7 4.4 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
66964555 117540 0 None -38 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 496 8 0 5 5.0 COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260536 117540 0 None -38 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 496 8 0 5 5.0 COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
89995611 160208 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 432 5 0 5 4.2 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3C#N)cc2)C2CC2)CC1 nan
CHEMBL3979128 160208 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 432 5 0 5 4.2 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccncc3C#N)cc2)C2CC2)CC1 nan
86709924 120706 0 None -6 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 5 0 9 3.3 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325844 120706 0 None -6 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 5 0 9 3.3 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
53492264 129074 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598100 129074 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 495 6 0 8 3.1 C[C@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
57397674 77603 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 386 5 0 7 3.7 Cc1ccncc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951017 77603 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 386 5 0 7 3.7 Cc1ccncc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
76317690 111851 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 458 5 0 6 4.2 CC(C)OC(=O)N1CCC(Oc2cccc(N3CCc4cc(S(C)(=O)=O)ccc43)c2)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113838 111851 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 458 5 0 6 4.2 CC(C)OC(=O)N1CCC(Oc2cccc(N3CCc4cc(S(C)(=O)=O)ccc43)c2)CC1 10.1016/j.bmc.2014.01.028
118722583 122945 0 None -5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 7 1 10 3.5 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=N)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358008 122945 0 None -5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 7 1 10 3.5 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=N)=O)cc2F)cn1 10.1021/jm5011012
139437014 180308 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 425 8 1 8 1.4 O=C(O)C1CN(c2ncc(N3CC[C@@H](Oc4ccc(OCC5CC5)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
CHEMBL4531290 180308 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 425 8 1 8 1.4 O=C(O)C1CN(c2ncc(N3CC[C@@H](Oc4ccc(OCC5CC5)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
72946094 111390 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104862 111390 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
54591108 157035 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 6 1 7 2.7 O=C1NN=C(c2ccc3nc(-c4ccc(OCCN5CCOCC5)cc4)oc3c2)C2CC12 nan
CHEMBL3952446 157035 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 6 1 7 2.7 O=C1NN=C(c2ccc3nc(-c4ccc(OCCN5CCOCC5)cc4)oc3c2)C2CC12 nan
71519193 93120 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 486 5 0 8 2.8 CCc1cnc(N2CCC([N+]3([O-])Cc4cn(-c5ccc(S(C)(=O)=O)cc5F)nc4C3)CC2)nc1 10.1016/j.bmcl.2012.10.119
CHEMBL2313413 93120 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 486 5 0 8 2.8 CCc1cnc(N2CCC([N+]3([O-])Cc4cn(-c5ccc(S(C)(=O)=O)cc5F)nc4C3)CC2)nc1 10.1016/j.bmcl.2012.10.119
51030053 84191 1 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmc.2022.116614
CHEMBL2086680 84191 1 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmc.2022.116614
54580747 68166 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 434 4 0 6 3.7 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1770161 68166 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 434 4 0 6 3.7 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
122194420 130792 0 None 9 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 6 1 9 3.3 COc1c(Nc2ccc(C#N)cc2F)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629597 130792 0 None 9 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 483 6 1 9 3.3 COc1c(Nc2ccc(C#N)cc2F)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
145975486 170774 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 418 8 0 4 5.0 CN(C)C(=O)c1ccc(OCCCCCC2CCN(C(=O)OC(C)(C)C)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4208239 170774 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 418 8 0 4 5.0 CN(C)C(=O)c1ccc(OCCCCCC2CCN(C(=O)OC(C)(C)C)CC2)cc1 10.1016/j.bmcl.2018.02.044
155566114 182514 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 475 4 0 7 4.2 CC1(C)C[C@]2(CC[C@H](Oc3ncnc4c3CCN4c3ccc(S(C)(=O)=O)cc3F)CC2)CO1 10.1016/j.bmcl.2018.12.041
CHEMBL4582928 182514 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 475 4 0 7 4.2 CC1(C)C[C@]2(CC[C@H](Oc3ncnc4c3CCN4c3ccc(S(C)(=O)=O)cc3F)CC2)CO1 10.1016/j.bmcl.2018.12.041
68211777 117665 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 528 8 0 6 4.6 CCCc1cnc(N2CCC(C3Cc4c(ccc(C5=CCN(S(=O)(=O)CCC)CC5)c4F)O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261134 117665 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 528 8 0 6 4.6 CCCc1cnc(N2CCC(C3Cc4c(ccc(C5=CCN(S(=O)(=O)CCC)CC5)c4F)O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
91824767 122682 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 500 5 2 7 3.8 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354798 122682 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 500 5 2 7 3.8 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354801 122682 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 500 5 2 7 3.8 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(CO)nn3c21 10.1016/j.bmcl.2014.10.010
51030054 84194 0 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086684 84194 0 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
51030054 84194 0 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086684 84194 0 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
51030897 84237 0 None 18 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2087086 84237 0 None 18 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
54587813 68369 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771098 68369 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
155531494 178441 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 484 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4466171 178441 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 484 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
145969910 171777 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 432 5 0 10 2.1 N#Cc1cnccc1COc1cnc(N2CCN(c3nc(C(F)(F)F)no3)CC2)nc1 10.1016/j.bmc.2018.04.004
CHEMBL4225726 171777 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 432 5 0 10 2.1 N#Cc1cnccc1COc1cnc(N2CCN(c3nc(C(F)(F)F)no3)CC2)nc1 10.1016/j.bmc.2018.04.004
51030054 84194 0 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL2086684 84194 0 None 23 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
25053112 183724 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 7 1 11 3.4 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1016/j.bmcl.2011.03.007
CHEMBL462196 183724 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 7 1 11 3.4 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1016/j.bmcl.2011.03.007
145949313 169673 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 485 5 1 7 5.3 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CCC1 10.1021/acsmedchemlett.8b00073
CHEMBL4173664 169673 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 485 5 1 7 5.3 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CCC1 10.1021/acsmedchemlett.8b00073
89583933 164400 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 455 8 0 6 3.6 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4081159 164400 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 455 8 0 6 3.6 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1)N1CCC1 10.1016/j.bmcl.2017.01.091
122191630 130515 0 None -1 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622172 130515 0 None -1 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 463 9 0 7 3.2 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
68230358 129078 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 461 7 0 7 2.6 CCC(F)(F)C(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598104 129078 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 461 7 0 7 2.6 CCC(F)(F)C(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
137649810 164167 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 536 6 2 10 3.9 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4078300 164167 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 536 6 2 10 3.9 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
164609330 191210 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 531 7 0 10 2.5 CS(=O)(=O)N1CCC(Oc2cc(N(C3CCN(c4nc(C5CC5)no4)CC3)C(F)(F)F)ncn2)CC1 10.1016/j.bmc.2021.116208
CHEMBL4846307 191210 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 531 7 0 10 2.5 CS(=O)(=O)N1CCC(Oc2cc(N(C3CCN(c4nc(C5CC5)no4)CC3)C(F)(F)F)ncn2)CC1 10.1016/j.bmc.2021.116208
57402128 77366 0 None 50 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 400 5 0 7 4.0 Cc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
CHEMBL1949674 77366 0 None 50 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 400 5 0 7 4.0 Cc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
71140721 130517 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 447 8 0 6 3.7 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622174 130517 0 None -2 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 447 8 0 6 3.7 CCc1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
21897897 68601 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 489 4 0 9 3.7 CC(C)(C)OC(=O)N1CCC(Sc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773282 68601 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 489 4 0 9 3.7 CC(C)(C)OC(=O)N1CCC(Sc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
137637825 162850 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 518 6 2 10 3.7 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4062726 162850 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 518 6 2 10 3.7 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
137632132 163307 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 523 6 1 10 3.4 CC(C)(C)OC(=O)N1CC2CC1CC2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4067982 163307 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 523 6 1 10 3.4 CC(C)(C)OC(=O)N1CC2CC1CC2Oc1ncnc(Nc2ccc(S(C)(=O)=O)cc2F)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
25053112 183724 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 487 7 1 11 3.4 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL462196 183724 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 487 7 1 11 3.4 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(C)(=O)=O)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
86717800 130523 0 None -1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 481 9 0 7 3.4 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3cc(F)c(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622180 130523 0 None -1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 481 9 0 7 3.4 COCc1cnc(N2CCC([C@H]3C[C@H]3COCc3cc(F)c(S(C)(=O)=O)c(F)c3)CC2)nc1 10.1021/acsmedchemlett.5b00207
53492594 129063 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598090 129063 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
71655178 97522 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 446 7 1 6 4.8 CCOC(=O)c1cc(C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
CHEMBL2391592 97522 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 446 7 1 6 4.8 CCOC(=O)c1cc(C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1 10.1016/j.bmcl.2013.04.014
76321322 111693 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 558 5 0 7 6.7 CC(C)(C)c1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
CHEMBL3112985 111693 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 558 5 0 7 6.7 CC(C)(C)c1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
76314044 111709 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 544 6 0 7 6.5 CC(C)c1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
CHEMBL3113001 111709 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 544 6 0 7 6.5 CC(C)c1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
76324931 111710 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113002 111710 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76320657 110017 0 None 5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 474 6 0 7 4.0 Cc1c(Oc2ccc(Cl)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084384 110017 0 None 5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 474 6 0 7 4.0 Cc1c(Oc2ccc(Cl)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
57402865 77613 0 None 13 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 477 7 1 9 3.3 CCc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951028 77613 0 None 13 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 477 7 1 9 3.3 CCc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
67466198 160100 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 326 2 1 6 2.5 CCC1OC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
CHEMBL3978218 160100 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 326 2 1 6 2.5 CCC1OC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
21897744 89301 28 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 211 2 1 5 1.2 CC(C)c1noc(N2CCC(O)CC2)n1 10.1021/jm301404a
CHEMBL2177769 89301 28 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 211 2 1 5 1.2 CC(C)c1noc(N2CCC(O)CC2)n1 10.1021/jm301404a
23653563 89309 12 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 478 5 0 8 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177777 89309 12 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 478 5 0 8 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
58016989 89837 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 7 0 8 3.5 CCCCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181693 89837 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 492 7 0 8 3.5 CCCCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
73357217 100014 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 462 5 0 7 3.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc([S@+](C)[O-])c(F)c2)CC1 10.1021/jm301404a
CHEMBL2448136 100014 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 462 5 0 7 3.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc([S@+](C)[O-])c(F)c2)CC1 10.1021/jm301404a
51030711 84200 4 None -23 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
CHEMBL2086690 84200 4 None -23 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
89995532 158659 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 2 7 4.0 CNC(=O)Nc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)ns1 nan
CHEMBL3965744 158659 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 2 7 4.0 CNC(=O)Nc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)ns1 nan
10166 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2014.03.023
25025505 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2014.03.023
CHEMBL3260505 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2014.03.023
DB12345 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2014.03.023
58017027 89308 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 458 5 0 6 4.2 CC(C)OC(=O)N1CCC(Oc2cccc3c2CCN3c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
CHEMBL2177776 89308 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 458 5 0 6 4.2 CC(C)OC(=O)N1CCC(Oc2cccc3c2CCN3c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
71461092 89833 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 473 6 0 8 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc([S+]([O-])N(C)C)cc2)CC1 10.1021/jm301404a
CHEMBL2181688 89833 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 473 6 0 8 3.1 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc([S+]([O-])N(C)C)cc2)CC1 10.1021/jm301404a
58017023 89840 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 482 6 0 8 2.7 CS(=O)(=O)c1ccc(N2CCc3c(OC4CCN(C(=O)OCCF)CC4)ncnc32)c(F)c1 10.1021/jm301404a
CHEMBL2181696 89840 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 482 6 0 8 2.7 CS(=O)(=O)c1ccc(N2CCc3c(OC4CCN(C(=O)OCCF)CC4)ncnc32)c(F)c1 10.1021/jm301404a
90666914 116237 0 None 6 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)O[C@@H]2CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220242 116237 0 None 6 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)O[C@@H]2CCOC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
90666911 116233 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 452 6 0 9 2.4 CC(C)C1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
CHEMBL3220238 116233 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 452 6 0 9 2.4 CC(C)C1(OC(=O)N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)COC1 10.1039/C2MD20130E
66554587 93758 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 419 5 0 4 6.1 CSc1ccc([C@H]2CC[C@H](OCC3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1021/ml300399u
CHEMBL2323598 93758 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 419 5 0 4 6.1 CSc1ccc([C@H]2CC[C@H](OCC3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1021/ml300399u
71736721 141714 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 496 5 0 5 5.6 CS(=O)(=O)c1ccc(-c2cc3cc(C4CCN(CC5(C(F)(F)F)CC5)CC4)oc3cn2)c(F)c1 nan
CHEMBL3719228 141714 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 496 5 0 5 5.6 CS(=O)(=O)c1ccc(-c2cc3cc(C4CCN(CC5(C(F)(F)F)CC5)CC4)oc3cn2)c(F)c1 nan
164612492 192025 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 527 6 0 8 4.2 CC(C)(C)OC(=O)N1CCC(N(CC2CC2)c2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116208
CHEMBL4858330 192025 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 527 6 0 8 4.2 CC(C)(C)OC(=O)N1CCC(N(CC2CC2)c2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116208
68240486 130773 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 2.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(S(=O)(=O)C1CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629480 130773 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 2.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(S(=O)(=O)C1CC1)C2 10.1016/j.bmcl.2015.09.047
54589232 117656 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 516 6 0 5 5.0 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(C(=O)OC4CCCCC4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261125 117656 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 516 6 0 5 5.0 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(C(=O)OC4CCCCC4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
62706030 83084 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 378 7 1 5 4.3 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058673 83084 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 378 7 1 5 4.3 CCc1cnc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)nc1 10.1016/j.bmcl.2012.05.117
51030901 84203 0 None -25 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2noc(C(F)(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086693 84203 0 None -25 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2noc(C(F)(F)F)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
89995720 156529 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 491 6 1 4 5.1 CCNC(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
CHEMBL3948147 156529 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 491 6 1 4 5.1 CCNC(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cc1 nan
54590845 149530 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 532 6 1 7 5.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCN(C(=O)OC(C)(C)C)CC4)cc3)oc2c1 nan
CHEMBL3892506 149530 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 532 6 1 7 5.8 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCN(C(=O)OC(C)(C)C)CC4)cc3)oc2c1 nan
54591405 166613 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 419 5 1 6 4.3 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOCC4)cc3)oc2c1 nan
CHEMBL4106479 166613 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 419 5 1 6 4.3 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOCC4)cc3)oc2c1 nan
70796891 117525 0 None -11 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260518 117525 0 None -11 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assayAgonist activity at GPR119 in mouse GLUTag cells assessed as stimulation of GLP1 secretion by CRE-luciferase reporter gene assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
54591870 166707 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 5 4.0 Cc1ccc(-c2nc3ccc(C4=NNC(=O)[C@@H](C)[C@H]4C)cc3o2)s1 nan
CHEMBL4107192 166707 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 339 2 1 5 4.0 Cc1ccc(-c2nc3ccc(C4=NNC(=O)[C@@H](C)[C@H]4C)cc3o2)s1 nan
145970094 171629 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 401 8 0 3 5.8 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CCC(C)(C)O3)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4218978 171629 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 401 8 0 3 5.8 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CCC(C)(C)O3)CC2)cc1 10.1016/j.bmcl.2018.02.044
62706354 83007 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 424 5 1 6 3.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058396 83007 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 424 5 1 6 3.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
68240224 130776 0 None -7 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 520 6 1 9 3.4 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CC2COCC(C1)N2C(=O)OC1(C)CC1 10.1016/j.bmcl.2015.09.047
CHEMBL3629483 130776 0 None -7 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 520 6 1 9 3.4 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CC2COCC(C1)N2C(=O)OC1(C)CC1 10.1016/j.bmcl.2015.09.047
137651954 164261 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 476 4 0 9 3.5 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncccn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
CHEMBL4079439 164261 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 476 4 0 9 3.5 CS(=O)(=O)c1ccc2c(c1)CCN2c1ncnc2c(C3CCN(c4ncccn4)CC3)coc12 10.1016/j.bmcl.2017.06.034
54583892 68345 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 390 3 0 4 5.3 CSc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771072 68345 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 390 3 0 4 5.3 CSc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
118300918 161070 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 6 4.0 Cc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)o1 nan
CHEMBL3986568 161070 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 426 4 0 6 4.0 Cc1nnc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)o1 nan
11462546 9997 43 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR119 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR119 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 10.1021/acsmedchemlett.6b00025
3319 9997 43 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR119 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR119 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 10.1021/acsmedchemlett.6b00025
CHEMBL1081913 9997 43 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR119 (unknown origin) by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR119 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 10.1021/acsmedchemlett.6b00025
24961071 68338 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 2 0 3 4.9 Cc1cccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)c1 10.1016/j.bmcl.2010.12.086
CHEMBL1771066 68338 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 2 0 3 4.9 Cc1cccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)c1 10.1016/j.bmcl.2010.12.086
62706516 83013 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CNC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058401 83013 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CNC3=O)CC1 10.1016/j.bmcl.2012.05.117
68036822 169881 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 517 6 1 9 3.4 CC1(COC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)COC1 10.1021/acsmedchemlett.8b00073
CHEMBL4177077 169881 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 517 6 1 9 3.4 CC1(COC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)COC1 10.1021/acsmedchemlett.8b00073
73388333 158435 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 439 5 0 6 3.7 O=C(OC1CCOCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3963959 158435 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 439 5 0 6 3.7 O=C(OC1CCOCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
68229751 129057 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)c(F)c3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598084 129057 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)c(F)c3)CC2)CC1 10.1016/j.bmcl.2015.04.102
68021978 147763 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 443 4 1 6 3.7 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4cc(F)c(C(N)=O)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823398 147763 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 443 4 1 6 3.7 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4cc(F)c(C(N)=O)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
76684031 171942 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 406 7 1 4 4.1 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(N)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4228188 171942 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 406 7 1 4 4.1 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(N)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
62706515 83012 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058400 83012 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCC3=O)CC1 10.1016/j.bmcl.2012.05.117
76320659 110023 0 None -2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 410 5 0 7 4.0 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084390 110023 0 None -2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 410 5 0 7 4.0 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@H]3C=C[C@@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
73387916 154716 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 409 5 0 5 4.1 CC1(OC(=O)N2CCC(N(C(=O)c3ccc(-c4cnco4)cc3)C3CC3)CC2)CC1 nan
CHEMBL3933770 154716 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 409 5 0 5 4.1 CC1(OC(=O)N2CCC(N(C(=O)c3ccc(-c4cnco4)cc3)C3CC3)CC2)CC1 nan
67466218 149864 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 453 7 1 5 6.0 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCc5ccccc5)cc4)oc3c2)[C@H]1C nan
CHEMBL3895341 149864 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 453 7 1 5 6.0 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCc5ccccc5)cc4)oc3c2)[C@H]1C nan
54591488 167709 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 6 1 7 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@H]4CCCN4C(=O)OC(C)(C)C)cc3)oc2c1 nan
CHEMBL4115415 167709 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 6 1 7 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC[C@H]4CCCN4C(=O)OC(C)(C)C)cc3)oc2c1 nan
76310464 111856 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 461 5 0 9 2.4 CC(C)OC(=O)N1CCC(Oc2ncnc(N3CCc4cc(S(C)(=O)=O)ccc43)n2)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113842 111856 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 461 5 0 9 2.4 CC(C)OC(=O)N1CCC(Oc2ncnc(N3CCc4cc(S(C)(=O)=O)ccc43)n2)CC1 10.1016/j.bmc.2014.01.028
54589229 117653 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 480 7 0 4 4.7 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(Cc4ccccc4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261122 117653 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 480 7 0 4 4.7 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(Cc4ccccc4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
54580903 68349 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ncccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771077 68349 0 None -1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ncccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
54580903 68349 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ncccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771077 68349 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 346 2 0 5 3.3 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ncccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
56592326 166052 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 498 3 0 8 4.4 CC(C)(C)OC(=O)N1CCC(c2coc3c(N4CCc5cc(S(C)(=O)=O)ccc54)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL4099307 166052 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 498 3 0 8 4.4 CC(C)(C)OC(=O)N1CCC(c2coc3c(N4CCc5cc(S(C)(=O)=O)ccc54)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
137656527 166533 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 529 5 0 8 5.0 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1F 10.1016/j.bmcl.2017.06.032
CHEMBL4105014 166533 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 529 5 0 8 5.0 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1F 10.1016/j.bmcl.2017.06.032
137650572 164214 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 522 6 2 10 3.5 CC(C)(C)OC(=O)N1CC2CC(Nc3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
CHEMBL4078851 164214 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 522 6 2 10 3.5 CC(C)(C)OC(=O)N1CC2CC(Nc3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
66964831 117546 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 424 6 0 5 5.8 CCOC(=O)C(C)(Cc1ccccc1)c1csc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260542 117546 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 424 6 0 5 5.8 CCOC(=O)C(C)(Cc1ccccc1)c1csc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
70689386 79834 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 476 6 0 6 3.5 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)c(F)c2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010840 79834 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 476 6 0 6 3.5 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)c(F)c2)CC1 10.1016/j.bmcl.2011.10.033
76309732 110008 0 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 432 7 0 7 3.4 CCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
CHEMBL3084375 110008 0 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 432 7 0 7 3.4 CCCS(=O)(=O)N1[C@H]2CC[C@@H]1C[C@H](Oc1ncnc(Oc3cccnc3C)c1C)C2 10.1016/j.bmcl.2011.04.035
53630415 68865 0 None -13 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 445 5 0 9 2.2 CCOC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775170 68865 0 None -13 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 445 5 0 9 2.2 CCOC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
67463297 151111 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 10 1 6 5.9 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN(C(C)C)C(C)C)cc4)oc3c2)[C@H]1C nan
CHEMBL3905505 151111 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 490 10 1 6 5.9 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCN(C(C)C)C(C)C)cc4)oc3c2)[C@H]1C nan
67464829 166828 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 4.8 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(C)s4)oc3c2)[C@@H]1C nan
CHEMBL4108252 166828 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 4.8 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(C)s4)oc3c2)[C@@H]1C nan
118720427 122684 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 528 5 2 7 4.5 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(C(C)(C)O)nn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354800 122684 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 528 5 2 7 4.5 COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(-c4ccc(C(F)(F)F)cc4)c(C(C)(C)O)nn3c21 10.1016/j.bmcl.2014.10.010
76328549 111803 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 486 4 0 6 4.3 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3c2ccc(S(C)(=O)=O)c3Cl)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113632 111803 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 486 4 0 6 4.3 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3c2ccc(S(C)(=O)=O)c3Cl)CC1 10.1016/j.bmc.2014.01.028
57397675 77604 1 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 390 5 0 7 3.5 Cc1c(Oc2cncc(F)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951018 77604 1 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 390 5 0 7 3.5 Cc1c(Oc2cncc(F)c2)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
60155100 84168 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
CHEMBL2086655 84168 0 None 1 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
70693583 79830 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 447 6 1 3 4.3 CC(=O)Nc1ccc(CC(=O)N(C)C2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmcl.2011.10.033
CHEMBL2010835 79830 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 447 6 1 3 4.3 CC(=O)Nc1ccc(CC(=O)N(C)C2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmcl.2011.10.033
70680969 79825 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 482 7 0 4 4.2 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010830 79825 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 482 7 0 4 4.2 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
67466400 152202 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 306 2 2 4 2.9 CC1NC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3914133 152202 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 306 2 2 4 2.9 CC1NC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
102361261 147249 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 588 6 0 6 6.1 C[C@@H](OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1016/j.bmcl.2018.08.010
CHEMBL3809509 147249 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 588 6 0 6 6.1 C[C@@H](OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1016/j.bmcl.2018.08.010
76324301 110018 0 None 37 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 429 6 1 7 3.1 Cc1ncccc1Nc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084385 110018 0 None 37 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 429 6 1 7 3.1 Cc1ncccc1Nc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
102361261 147249 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assayAgonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assay
ChEMBL 588 6 0 6 6.1 C[C@@H](OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1021/acs.jmedchem.5b01198
CHEMBL3809509 147249 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assayAgonist activity at human GPR119 receptor assessed as increase in cellular cAMP levels by HTRF assay
ChEMBL 588 6 0 6 6.1 C[C@@H](OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccn5)cc4)ccc3O2)CC1)C(F)(F)F 10.1021/acs.jmedchem.5b01198
58190423 84173 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CCN1C(=O)OC(C)(C)C 10.1021/jm300310c
CHEMBL2086661 84173 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CCN1C(=O)OC(C)(C)C 10.1021/jm300310c
58190347 84174 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CCN1C(=O)OC(C)(C)C 10.1021/jm300310c
CHEMBL2086662 84174 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CCN1C(=O)OC(C)(C)C 10.1021/jm300310c
51030529 84196 0 None 19 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 421 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C#N)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086686 84196 0 None 19 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 421 5 0 9 2.3 C[C@@H]1CN(C(=O)OC(C)(C)C#N)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
53491781 129064 0 None -2 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 483 6 0 8 3.8 CC(C)S(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598091 129064 0 None -2 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 483 6 0 8 3.8 CC(C)S(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C)(C)C)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
67462782 159338 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4C[C@H](C)O[C@H](C)C4)cc3)oc2c1 nan
CHEMBL3971716 159338 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4C[C@H](C)O[C@H](C)C4)cc3)oc2c1 nan
53492463 129083 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 491 7 0 7 3.8 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598109 129083 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 491 7 0 7 3.8 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
76314047 111716 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1cccc(Cl)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113008 111716 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1cccc(Cl)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
90656529 117662 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 495 6 0 6 4.9 CCCc1cnc(N2CCC(C3Cc4cc(-c5ccc(S(C)(=O)=O)cc5F)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261131 117662 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 495 6 0 6 4.9 CCCc1cnc(N2CCC(C3Cc4cc(-c5ccc(S(C)(=O)=O)cc5F)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
54589190 117663 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 513 8 0 7 3.5 CCCc1cnc(N2CCC(C3Cc4cc(N5CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261132 117663 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 513 8 0 7 3.5 CCCc1cnc(N2CCC(C3Cc4cc(N5CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
67462437 154513 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)(C)CN4CCCC4)cc3)oc2c1 nan
CHEMBL3932264 154513 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)(C)CN4CCCC4)cc3)oc2c1 nan
76683707 171917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 451 5 0 5 5.1 CC(C)(C)OC(=O)N1CCC2(CCC(CCOc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmc.2018.02.032
CHEMBL4227805 171917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 451 5 0 5 5.1 CC(C)(C)OC(=O)N1CCC2(CCC(CCOc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmc.2018.02.032
118722571 122931 0 None 36 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 523 6 0 11 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm5011012
CHEMBL3357995 122931 0 None 36 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 523 6 0 11 2.4 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2C#N)cn1 10.1021/jm5011012
76327867 109998 0 None -2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 5 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084364 109998 0 None -2 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 5 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C)c1C 10.1016/j.bmcl.2011.04.035
11503692 77598 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951011 77598 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
118300929 152784 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 452 5 0 6 4.2 COc1ncc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
CHEMBL3918525 152784 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 452 5 0 6 4.2 COc1ncc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
76314046 111714 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 533 6 0 8 5.5 N#Cc1cccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)c1 10.1016/j.bmcl.2013.12.127
CHEMBL3113006 111714 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 533 6 0 8 5.5 N#Cc1cccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)c1 10.1016/j.bmcl.2013.12.127
62706516 83013 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CNC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058401 83013 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CNC3=O)CC1 10.1016/j.bmcl.2012.05.117
54590843 151173 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 420 8 1 6 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCCN(C)C)cc3)oc2c1 nan
CHEMBL3906013 151173 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 420 8 1 6 4.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCCN(C)C)cc3)oc2c1 nan
67464510 153386 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 458 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4C[C@H]5CC[C@@H]4C5)cc3)oc2c1 nan
CHEMBL3923217 153386 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 458 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4C[C@H]5CC[C@@H]4C5)cc3)oc2c1 nan
71545378 93025 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 409 4 0 7 3.6 CCOC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
CHEMBL2312521 93025 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 409 4 0 7 3.6 CCOC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
54586548 68996 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 4 0 7 4.1 Cc1ncccc1Oc1ncnc(O[C@@H]2CC3CC2CN3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778134 68996 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 4 0 7 4.1 Cc1ncccc1Oc1ncnc(O[C@@H]2CC3CC2CN3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
71545377 93024 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 423 4 0 7 4.0 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)C)c1C 10.1021/jm301626p
CHEMBL2312520 93024 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 423 4 0 7 4.0 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)C)c1C 10.1021/jm301626p
71081352 173512 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 547 5 0 5 6.6 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4283180 173512 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 547 5 0 5 6.6 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccccc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
51030711 84200 4 None -23 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2086690 84200 4 None -23 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
51030711 84200 4 None -23 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1021/jm300310c
CHEMBL2086690 84200 4 None -23 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1021/jm300310c
54591103 150658 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 4 1 4 4.4 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3901814 150658 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 4 1 4 4.4 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
66963944 117517 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 492 6 0 7 4.9 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(C3CCN(C(=O)OC(C)(C)C)CC3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260508 117517 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 492 6 0 7 4.9 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(C3CCN(C(=O)OC(C)(C)C)CC3)cnn12 10.1016/j.bmcl.2014.03.023
71736570 141630 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 512 5 0 6 7.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C(=O)OCc5ccccc5)cc4)ncc3o2)CC1 nan
CHEMBL3718900 141630 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 512 5 0 6 7.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(C(=O)OCc5ccccc5)cc4)ncc3o2)CC1 nan
51030056 84199 0 None -8 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 406 5 0 9 2.0 C[C@@H]1CN(c2ncc(F)cn2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086689 84199 0 None -8 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 406 5 0 9 2.0 C[C@@H]1CN(c2ncc(F)cn2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
54591182 150379 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCCCCC4)c3)oc2c1 nan
CHEMBL3899491 150379 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCCCCC4)c3)oc2c1 nan
66556122 93757 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 437 6 0 5 4.4 CC(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1021/ml300399u
CHEMBL2323597 93757 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 437 6 0 5 4.4 CC(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1021/ml300399u
54583894 68358 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 4 0 6 3.3 Cc1cnc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771086 68358 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 4 0 6 3.3 Cc1cnc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
137660484 166105 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 516 5 0 8 4.9 CON(C)C(=O)c1ccc(-c2csc3c(OC4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1F 10.1016/j.bmcl.2017.06.032
CHEMBL4099911 166105 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 516 5 0 8 4.9 CON(C)C(=O)c1ccc(-c2csc3c(OC4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1F 10.1016/j.bmcl.2017.06.032
139437017 180538 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 421 7 1 8 1.5 N#Cc1cc(N2CC[C@@H](Oc3ccc(OCC4CC4)nc3)C2=O)cnc1N1CC(O)C1 10.1021/acsmedchemlett.8b00622
CHEMBL4537090 180538 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 421 7 1 8 1.5 N#Cc1cc(N2CC[C@@H](Oc3ccc(OCC4CC4)nc3)C2=O)cnc1N1CC(O)C1 10.1021/acsmedchemlett.8b00622
89995615 149363 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 512 6 0 5 4.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(CS(C)(=O)=O)cc3)cc2)C2CC2)CC1 nan
CHEMBL3891199 149363 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 512 6 0 5 4.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(CS(C)(=O)=O)cc3)cc2)C2CC2)CC1 nan
67467075 151468 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 326 2 1 6 2.5 CC[C@@H]1OC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
CHEMBL3908474 151468 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 326 2 1 6 2.5 CC[C@@H]1OC(=O)NN=C1N1CCc2nc(-c3ccccc3)oc2C1 nan
67973622 140831 1 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 456 3 0 6 5.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc3o2)CC1 nan
CHEMBL3716247 140831 1 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 456 3 0 6 5.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4)ncc3o2)CC1 nan
118722579 122940 0 None 16 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
CHEMBL3358003 122940 0 None 16 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
87217189 117536 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 420 6 0 6 4.5 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)nc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260531 117536 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 420 6 0 6 4.5 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)nc3)cnn12 10.1016/j.bmcl.2014.03.023
62707006 83085 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 6 4.4 CC(C)c1noc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1016/j.bmcl.2012.05.117
CHEMBL2058674 83085 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 6 4.4 CC(C)c1noc(N2CCC(CCCNc3ccc4c(c3)C(=O)CC4)CC2)n1 10.1016/j.bmcl.2012.05.117
145957126 168803 0 None -5 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 487 5 1 8 3.9 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4159767 168803 0 None -5 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 487 5 1 8 3.9 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
88567661 169173 0 None -3 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 463 5 1 8 3.4 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3cccnc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4165734 169173 0 None -3 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 463 5 1 8 3.4 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3cccnc3Cl)c2F)CC1 10.1021/acsmedchemlett.8b00073
118722576 122937 0 None -8 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 506 6 0 12 2.3 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2F)cn1 10.1021/jm5011012
CHEMBL3358000 122937 0 None -8 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 506 6 0 12 2.3 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2F)cn1 10.1021/jm5011012
67465252 154895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 10 1 6 5.2 CCCN(CCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1)C(C)C nan
CHEMBL3935285 154895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 10 1 6 5.2 CCCN(CCOc1ccc(-c2nc3ccc(C4=NNC(=O)CC4CC)cc3o2)cc1)C(C)C nan
54591955 160723 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 411 5 1 5 4.9 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccccc4)cc3)oc2c1 nan
CHEMBL3983527 160723 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 411 5 1 5 4.9 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccccc4)cc3)oc2c1 nan
137642901 164866 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 520 5 1 10 3.5 CC(O)c1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
CHEMBL4086445 164866 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 520 5 1 10 3.5 CC(O)c1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
155530128 178261 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 464 5 0 7 4.6 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4463622 178261 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 464 5 0 7 4.6 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
76327868 110003 0 None -1 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 438 6 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084369 110003 0 None -1 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 438 6 0 7 4.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OC(C)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
89995721 155124 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 437 5 0 5 4.9 O=C(OC1CCCCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3937113 155124 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 437 5 0 5 4.9 O=C(OC1CCCCC1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
67463444 158270 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)C)cc3)oc2c1 nan
CHEMBL3962398 158270 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)C)cc3)oc2c1 nan
76310377 111717 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 538 7 0 8 5.6 COc1cccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)c1 10.1016/j.bmcl.2013.12.127
CHEMBL3113009 111717 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 538 7 0 8 5.6 COc1cccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)c1 10.1016/j.bmcl.2013.12.127
67466546 156310 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CN4CCCC4)cc3)oc2c1 nan
CHEMBL3946567 156310 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 7 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)CN4CCCC4)cc3)oc2c1 nan
86694577 141638 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 369 2 0 6 4.6 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4cnco4)ncc3o2)CC1 nan
CHEMBL3718966 141638 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 369 2 0 6 4.6 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4cnco4)ncc3o2)CC1 nan
54591718 167312 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@@H]1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
CHEMBL4112376 167312 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@@H]1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
53322927 65336 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 360 5 1 3 3.6 CC(CNC(=O)Cc1ccccc1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684036 65336 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 360 5 1 3 3.6 CC(CNC(=O)Cc1ccccc1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
51030710 96978 0 None 70 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmc.2022.116614
CHEMBL2382416 96978 0 None 70 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmc.2022.116614
24961799 68351 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccnc(C#N)n3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771079 68351 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccnc(C#N)n3)CC2)CC1 10.1016/j.bmcl.2010.12.086
24961798 68352 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cc(C#N)ncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771080 68352 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 371 2 0 6 3.2 CC(C)(C)OC(=O)N1CCC(C2CCN(c3cc(C#N)ncn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
145962089 168889 0 None 4 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 446 5 1 7 3.5 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4161243 168889 0 None 4 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 446 5 1 7 3.5 CC1(OC(=O)N2C[C@H]3COC[C@@H](C2)[C@@H]3Oc2ncnc(Nc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
68036465 169295 0 None 7 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 485 6 1 8 3.8 CCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4167676 169295 0 None 7 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 485 6 1 8 3.8 CCC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
118722587 122951 0 None 10 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 490 7 0 10 2.8 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(S(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
CHEMBL3358014 122951 0 None 10 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 490 7 0 10 2.8 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(S(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
118720432 122687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 483 5 2 6 4.4 OCc1nn2c3c(cnc2c1-c1ccc(C(F)(F)F)nc1)CN[C@]3(Cc1cccc(F)c1)C1CC1 10.1016/j.bmcl.2014.10.010
CHEMBL3354805 122687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 483 5 2 6 4.4 OCc1nn2c3c(cnc2c1-c1ccc(C(F)(F)F)nc1)CN[C@]3(Cc1cccc(F)c1)C1CC1 10.1016/j.bmcl.2014.10.010
73353419 96974 0 None 39 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382412 96974 0 None 39 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
58190314 84183 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 452 5 0 10 2.5 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2)cn1 10.1021/jm300310c
CHEMBL2086671 84183 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 452 5 0 10 2.5 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2)cn1 10.1021/jm300310c
24939268 7240 67 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmc.2021.116071
5653 7240 67 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmc.2021.116071
CHEMBL461384 7240 67 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmc.2021.116071
44467185 68371 0 None -1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 7 0 7 4.0 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cc3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771101 68371 0 None -1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 7 0 7 4.0 Clc1cnc(N2CCC([C@H]3C[C@H]3CCOc3ccc(-n4ccnn4)cc3)CC2)nc1 10.1016/j.bmcl.2010.12.086
155549064 181022 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 506 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CCC(F)(F)CO2)CC1)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4548931 181022 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 506 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CCC(F)(F)CO2)CC1)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
118711798 120824 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 10 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3ncc(Cl)cn3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326689 120824 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 10 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3ncc(Cl)cn3)CC2)c1F 10.1016/j.bmcl.2014.06.071
134138752 154318 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 522 7 2 10 3.6 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
CHEMBL3930728 154318 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
ChEMBL 522 7 2 10 3.6 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Nc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmc.2016.10.030
53630398 68599 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 514 6 0 9 3.7 CCN(CC1CCN(C(=O)OC(C)(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1 10.1016/j.bmcl.2011.03.007
CHEMBL1773280 68599 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 514 6 0 9 3.7 CCN(CC1CCN(C(=O)OC(C)(C)C)CC1)c1ncnc2c1cnn2-c1ccc(S(C)(=O)=O)cc1 10.1016/j.bmcl.2011.03.007
66556297 93759 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 469 5 0 5 4.9 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1021/ml300399u
CHEMBL2323599 93759 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 469 5 0 5 4.9 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1021/ml300399u
137637825 162850 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 518 6 2 10 3.7 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
CHEMBL4062726 162850 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 518 6 2 10 3.7 CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(S(C)(=O)=O)cc2)c1[N+](=O)[O-] 10.1016/j.bmcl.2017.03.092
118711213 120708 0 None 7 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 536 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325846 120708 0 None 7 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 536 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
70855957 162810 0 None -1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 458 8 0 4 4.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)CC1 10.1016/j.bmcl.2017.01.091
CHEMBL4062339 162810 0 None -1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 458 8 0 4 4.4 CC1(OC(=O)N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)CC1 10.1016/j.bmcl.2017.01.091
71562726 110054 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 550 7 2 10 4.3 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](CNc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
CHEMBL3084481 110054 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamineAgonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
ChEMBL 550 7 2 10 4.3 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](CNc1ncnc(Nc3ccc(S(C)(=O)=O)cc3F)c1[N+](=O)[O-])C2 10.1016/j.bmcl.2012.12.011
89584012 164322 0 None -8 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 488 8 1 6 3.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CC(O)C1 10.1016/j.bmcl.2017.01.091
CHEMBL4080222 164322 0 None -8 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 488 8 1 6 3.3 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1F)N1CC(O)C1 10.1016/j.bmcl.2017.01.091
70856302 165891 0 None -3 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 470 9 0 6 4.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)n1 10.1016/j.bmcl.2017.01.091
CHEMBL4097638 165891 0 None -3 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 470 9 0 6 4.4 CC(C)c1noc(N2CCC([C@H]3C[C@H]3CCOc3ccc(CC(=O)N4CCC4)c(F)c3)CC2)n1 10.1016/j.bmcl.2017.01.091
76328564 111850 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 484 4 0 6 4.0 CC(COC(=O)N1CCc2cc(S(C)(=O)=O)cc(F)c21)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113837 111850 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 484 4 0 6 4.0 CC(COC(=O)N1CCc2cc(S(C)(=O)=O)cc(F)c21)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
118711780 120807 0 None 6 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326672 120807 0 None 6 2 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
137639896 163702 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 524 6 1 8 4.5 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(C(F)(F)F)c1 10.1016/j.bmc.2017.06.014
CHEMBL4072376 163702 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 524 6 1 8 4.5 CCNC(=O)c1ccc(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(C(F)(F)F)c1 10.1016/j.bmc.2017.06.014
76328494 111692 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 556 7 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(CC5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112984 111692 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 556 7 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nc(CC5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76328495 111702 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 578 6 0 8 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCOc2cc(Cl)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112994 111702 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 578 6 0 8 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCOc2cc(Cl)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76335815 111708 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 528 6 0 7 5.9 O=S(=O)(c1ccc(Cl)cc1)N1CCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113000 111708 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 528 6 0 7 5.9 O=S(=O)(c1ccc(Cl)cc1)N1CCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
54589149 117670 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 558 10 1 7 4.0 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCCCO)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261139 117670 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 558 10 1 7 4.0 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCCCO)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
57392379 77610 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1cc(S(C)(=O)=O)ncc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951024 77610 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 464 6 0 9 3.1 Cc1cc(S(C)(=O)=O)ncc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
57392380 77614 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 489 7 1 9 3.6 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C1CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951029 77614 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 489 7 1 9 3.6 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C1CC1 10.1016/j.bmcl.2011.12.092
68036931 168999 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 487 5 1 8 3.9 N#Cc1ccc(Nc2ncnc(OC3C4COCC3CN(C(=O)OC3CCC3)C4)c2F)c(Cl)c1 10.1021/acsmedchemlett.8b00073
CHEMBL4163003 168999 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 487 5 1 8 3.9 N#Cc1ccc(Nc2ncnc(OC3C4COCC3CN(C(=O)OC3CCC3)C4)c2F)c(Cl)c1 10.1021/acsmedchemlett.8b00073
68036809 169675 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 501 5 1 8 4.3 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CCC1 10.1021/acsmedchemlett.8b00073
CHEMBL4173709 169675 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 501 5 1 8 4.3 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Nc3ccc(C#N)cc3Cl)c2F)CCC1 10.1021/acsmedchemlett.8b00073
118722587 122951 0 None -10 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 490 7 0 10 2.8 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(S(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
CHEMBL3358014 122951 0 None -10 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 490 7 0 10 2.8 CC(C)c1noc(N2CCN(c3ncc(OCc4ccc(S(C)(=O)=O)cc4F)cn3)[C@H](C)C2)n1 10.1021/jm5011012
62706850 83078 0 None 1 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 7 3.2 COc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
CHEMBL2058667 83078 0 None 1 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 382 7 1 7 3.2 COc1cnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)nc1 10.1016/j.bmcl.2012.05.117
122184148 129087 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
CHEMBL3598113 129087 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
67461067 154130 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 5 1 7 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCN(C(=O)OC(C)(C)C)CC4)cc3)oc2c1 nan
CHEMBL3929405 154130 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 518 5 1 7 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCN(C(=O)OC(C)(C)C)CC4)cc3)oc2c1 nan
141750312 186540 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 583 8 2 10 2.5 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(c3nc(-c4ccccc4)c[nH]3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4744389 186540 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 583 8 2 10 2.5 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(c3nc(-c4ccccc4)c[nH]3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
54583892 68345 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 390 3 0 4 5.3 CSc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771072 68345 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 390 3 0 4 5.3 CSc1ccc(N2CCC(C3CCN(C(=O)OC(C)(C)C)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
67462539 150451 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C(C)C)C(C)C)cc3)oc2c1 nan
CHEMBL3900085 150451 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 462 9 1 6 5.2 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN(C(C)C)C(C)C)cc3)oc2c1 nan
67464684 155411 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)C)cc3)oc2c1 nan
CHEMBL3939384 155411 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.5 CC[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC(C)C)cc3)oc2c1 nan
118711796 120822 0 None -13 2 Rat 6.2 pEC50 = 6.2 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3nc(C(C)(C)F)no3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326687 120822 0 None -13 2 Rat 6.2 pEC50 = 6.2 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 538 7 0 11 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)c3nc(C(C)(C)F)no3)CC2)c1F 10.1016/j.bmcl.2014.06.071
137631474 163348 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 484 4 0 7 3.8 CC(C)OC(=O)N1CCC(n2nnc3cc(-c4cc(F)c(C(=O)N5CCC5)cc4F)ncc32)CC1 10.1016/j.bmc.2017.06.014
CHEMBL4068495 163348 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 484 4 0 7 3.8 CC(C)OC(=O)N1CCC(n2nnc3cc(-c4cc(F)c(C(=O)N5CCC5)cc4F)ncc32)CC1 10.1016/j.bmc.2017.06.014
76309730 110001 0 None 165 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 452 5 0 7 4.4 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084367 110001 0 None 165 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 452 5 0 7 4.4 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
53492528 129056 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598083 129056 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1016/j.bmcl.2015.04.102
67464523 150621 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 3.7 CCC1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3901563 150621 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 3.7 CCC1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
71655177 97470 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 498 8 1 6 5.0 CCN(CC)C(=O)c1cc(C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
CHEMBL2391436 97470 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 498 8 1 6 5.0 CCN(CC)C(=O)c1cc(C)nc(Oc2cccc(NS(=O)(=O)c3ccc(Cl)cc3)c2)c1C#N 10.1016/j.bmcl.2013.04.014
54590928 152310 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 3.7 CC[C@@H]1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3914988 152310 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 3 1 5 3.7 CC[C@@H]1OC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
71736412 140912 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 474 3 0 6 5.2 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)c(F)c4)ncc3o2)CC1 nan
CHEMBL3716518 140912 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 474 3 0 6 5.2 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)c(F)c4)ncc3o2)CC1 nan
54581961 68362 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 4 0 6 3.5 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C#N)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771091 68362 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 4 0 6 3.5 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C#N)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
54587592 69005 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 466 6 0 7 3.4 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778255 69005 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 466 6 0 7 3.4 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
54589151 117666 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 528 8 0 6 4.6 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCC)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261135 117666 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 528 8 0 6 4.6 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCC)CC5)cc(F)c4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
66964802 117545 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)ncn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260541 117545 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)ncn12 10.1016/j.bmcl.2014.03.023
89995724 156730 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 397 5 0 5 4.0 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3949822 156730 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 397 5 0 5 4.0 CC(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
67464929 158522 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 464 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCSCC4)cc3)oc2c1 nan
CHEMBL3964608 158522 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 464 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCSCC4)cc3)oc2c1 nan
53492397 129082 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 477 7 0 7 3.4 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598108 129082 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 477 7 0 7 3.4 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
51029603 84187 1 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 371 4 0 7 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086675 84187 1 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 371 4 0 7 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3)cn2)CC1 10.1021/jm300310c
67462405 151759 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 503 9 1 7 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(C)CC)CC4)cc3)oc2c1 nan
CHEMBL3910800 151759 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 503 9 1 7 4.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(C)CC)CC4)cc3)oc2c1 nan
67466238 154646 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 7 1 6 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCC4)cc3)oc2c1 nan
CHEMBL3933234 154646 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 432 7 1 6 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCCC4)cc3)oc2c1 nan
66554933 93762 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 392 4 0 4 4.9 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccncc3F)CC2)CC1 10.1021/ml300399u
CHEMBL2323602 93762 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 392 4 0 4 4.9 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3ccncc3F)CC2)CC1 10.1021/ml300399u
68022196 147740 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 456 3 0 7 4.1 CC(C)(C)OC(=O)N1CCC(n2nnc3cc(-c4ccc(S(C)(=O)=O)cc4)ccc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823123 147740 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 456 3 0 7 4.1 CC(C)(C)OC(=O)N1CCC(n2nnc3cc(-c4ccc(S(C)(=O)=O)cc4)ccc32)CC1 10.1016/j.bmcl.2016.06.050
76684133 171957 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 429 8 1 5 4.2 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NC3CC3)cn1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4228417 171957 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 429 8 1 5 4.2 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NC3CC3)cn1)C2 10.1016/j.bmc.2018.02.032
66964852 117531 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 427 6 0 6 4.7 CCOC(=O)C(C)(CC1CCOCC1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260525 117531 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 427 6 0 6 4.7 CCOC(=O)C(C)(CC1CCOCC1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
60155457 84190 0 None 18 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 389 4 0 7 2.6 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3F)cn2)CC1 10.1021/jm300310c
CHEMBL2086679 84190 0 None 18 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 389 4 0 7 2.6 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3F)cn2)CC1 10.1021/jm300310c
51030056 84199 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 406 5 0 9 2.0 C[C@@H]1CN(c2ncc(F)cn2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086689 84199 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 406 5 0 9 2.0 C[C@@H]1CN(c2ncc(F)cn2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
76320654 110007 0 None -2 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 430 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084374 110007 0 None -2 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 430 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
58017045 89314 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 425 4 0 7 3.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(C#N)cc2F)CC1 10.1021/jm301404a
CHEMBL2177782 89314 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 425 4 0 7 3.6 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(C#N)cc2F)CC1 10.1021/jm301404a
58190329 116195 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 448 6 0 11 1.7 C[C@@H]1CN(c2noc(C3(C)COC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220032 116195 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 448 6 0 11 1.7 C[C@@H]1CN(c2noc(C3(C)COC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
118711778 120805 0 None -4 2 Rat 7.2 pEC50 = 7.2 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 548 6 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326670 120805 0 None -4 2 Rat 7.2 pEC50 = 7.2 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 548 6 0 9 4.0 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC3(C(F)(F)F)CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
71455380 89310 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 4.8 CC(C)(C)OC(=O)N1CCC(Oc2cccc3c2ccn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
CHEMBL2177778 89310 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 470 4 0 6 4.8 CC(C)(C)OC(=O)N1CCC(Oc2cccc3c2ccn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1021/jm301404a
58016999 89825 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 8 3.2 CC(C)OC(=O)N1CCC(N(C)c2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181677 89825 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 8 3.2 CC(C)OC(=O)N1CCC(N(C)c2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
73348101 100017 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 462 5 0 7 3.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc([S@@+](C)[O-])c(F)c2)CC1 10.1021/jm301404a
CHEMBL2448159 100017 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 462 5 0 7 3.4 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc([S@@+](C)[O-])c(F)c2)CC1 10.1021/jm301404a
90666909 116230 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 6 1 11 1.6 C[C@@H]1CN(c2noc(C(C)(C)O)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220234 116230 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 6 1 11 1.6 C[C@@H]1CN(c2noc(C(C)(C)O)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
51030707 116236 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 438 5 0 9 2.1 C[C@@H]1CN(C(=O)OC2CCOCC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220241 116236 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 438 5 0 9 2.1 C[C@@H]1CN(C(=O)OC2CCOCC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
90666908 116229 0 None -6 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 464 6 0 12 1.5 C[C@@H]1CN(c2noc(C3COCCO3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220233 116229 0 None -6 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 464 6 0 12 1.5 C[C@@H]1CN(c2noc(C3COCCO3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
90666909 116230 0 None -1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 6 1 11 1.6 C[C@@H]1CN(c2noc(C(C)(C)O)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220234 116230 0 None -1 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 436 6 1 11 1.6 C[C@@H]1CN(c2noc(C(C)(C)O)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
90666913 116235 0 None -3 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)OC2(C)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
CHEMBL3220240 116235 0 None -3 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at mouse GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 424 5 0 9 1.8 C[C@@H]1CN(C(=O)OC2(C)COC2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1039/C2MD20130E
60155461 84198 0 None -6 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 8 2.2 C[C@@H]1CN(C(=O)OCC(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086688 84198 0 None -6 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 8 2.2 C[C@@H]1CN(C(=O)OCC(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
89995647 166984 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@H](F)C1 nan
CHEMBL4109583 166984 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.3 CC(C)(C)OC(=O)N1CC[C@@H](N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)[C@H](F)C1 nan
71545379 93026 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CC2)c1C 10.1021/jm301626p
CHEMBL2312522 93026 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CC2)c1C 10.1021/jm301626p
136088927 155197 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 2 5 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(O)cc3)oc2c1 nan
CHEMBL3937706 155197 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 2 5 3.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(O)cc3)oc2c1 nan
89995530 155909 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 5 3.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cccn3)cc2)C2CC2)CC1 nan
CHEMBL3943310 155909 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 5 3.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3cccn3)cc2)C2CC2)CC1 nan
67465153 150819 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CC(C)OC(C)C4)c3)oc2c1 nan
CHEMBL3903079 150819 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CC(C)OC(C)C4)c3)oc2c1 nan
68209612 154196 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cccnc4)cc3)oc2c1 nan
CHEMBL3929893 154196 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4cccnc4)cc3)oc2c1 nan
71736720 140529 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 480 5 0 7 4.8 CCc1cnc(N2CCC(c3cc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc4o3)CC2)nc1 nan
CHEMBL3715162 140529 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 480 5 0 7 4.8 CCc1cnc(N2CCC(c3cc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc4o3)CC2)nc1 nan
137642936 164924 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 498 5 0 8 4.8 CON(C)C(=O)c1ccc(-c2csc3c(OC4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1 10.1016/j.bmcl.2017.06.032
CHEMBL4087235 164924 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 498 5 0 8 4.8 CON(C)C(=O)c1ccc(-c2csc3c(OC4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1 10.1016/j.bmcl.2017.06.032
58190343 84176 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 C[C@H]1CN(C(=O)OC(C)(C)C)C[C@@H](C)N1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086664 84176 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 476 5 0 8 3.3 C[C@H]1CN(C(=O)OC(C)(C)C)C[C@@H](C)N1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
54586780 68367 0 None -3 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C)nc(C#N)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
CHEMBL1771096 68367 0 None -3 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C)nc(C#N)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
53492594 129063 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598090 129063 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
155514874 176674 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 484 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2cc(F)c(CS(C)(=O)=O)cc2F)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4440715 176674 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 484 6 0 7 4.8 C[C@@H](O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2cc(F)c(CS(C)(=O)=O)cc2F)no1 10.1016/j.bmcl.2019.07.004
122184149 129088 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
CHEMBL3598114 129088 0 None -2 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
24939268 7240 67 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.ejmech.2019.112017
5653 7240 67 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.ejmech.2019.112017
CHEMBL461384 7240 67 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.ejmech.2019.112017
76320656 110014 0 None -3 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 510 7 1 8 2.9 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084381 110014 0 None -3 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 510 7 1 8 2.9 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
51029601 84164 3 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmc.2022.116614
CHEMBL2086650 84164 3 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR119 (unknown origin)Agonist activity at GPR119 (unknown origin)
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmc.2022.116614
54584353 68008 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
168282787 197951 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 478 4 0 7 4.0 CC(C)OC(=O)N1CCC(n2ncc3ccc(-c4cc(F)c(S(C)(=O)=O)cc4F)nc32)CC1 10.1016/j.bmc.2022.116614
CHEMBL5188902 197951 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 478 4 0 7 4.0 CC(C)OC(=O)N1CCC(n2ncc3ccc(-c4cc(F)c(S(C)(=O)=O)cc4F)nc32)CC1 10.1016/j.bmc.2022.116614
132486941 165136 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 498 4 0 7 4.2 CC(C)OC(=O)N1CCC(n2nnc3cc(-c4cc(F)c(C(=O)N5CCCC5)cc4F)ncc32)CC1 10.1016/j.bmc.2017.06.014
CHEMBL4089628 165136 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 498 4 0 7 4.2 CC(C)OC(=O)N1CCC(n2nnc3cc(-c4cc(F)c(C(=O)N5CCCC5)cc4F)ncc32)CC1 10.1016/j.bmc.2017.06.014
122194339 130775 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 427 5 1 8 3.1 Cc1ncccc1Nc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1016/j.bmcl.2015.09.047
CHEMBL3629482 130775 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 427 5 1 8 3.1 Cc1ncccc1Nc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1016/j.bmcl.2015.09.047
51029601 84164 3 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086650 84164 3 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
51029601 84164 3 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086650 84164 3 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
21897675 68871 0 None -7 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 487 5 0 9 3.2 CC(C)(C)COC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775176 68871 0 None -7 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 487 5 0 9 3.2 CC(C)(C)COC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
53491780 129071 0 None 7 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 477 8 0 8 2.5 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(CF)CF)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598098 129071 0 None 7 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 477 8 0 8 2.5 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(CF)CF)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
118711216 120711 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 472 6 0 9 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325849 120711 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 472 6 0 9 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
141750311 186205 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 601 8 1 12 2.2 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3nc(-c4ccccc4)cs3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4740282 186205 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 601 8 1 12 2.2 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCN(c3nc(-c4ccccc4)cs3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
73388332 154416 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 441 5 0 6 4.4 COc1cc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)ccc1-c1cnco1 nan
CHEMBL3931436 154416 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 441 5 0 6 4.4 COc1cc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)ccc1-c1cnco1 nan
118300917 157429 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 412 4 0 6 3.7 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3nnco3)cc2)C2CC2)CC1 nan
CHEMBL3955532 157429 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 412 4 0 6 3.7 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3nnco3)cc2)C2CC2)CC1 nan
67450521 129066 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598093 129066 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)nn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
89995544 160416 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 421 4 0 4 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cccnc3)cc2)C2CC2)CC1 nan
CHEMBL3980921 160416 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 421 4 0 4 4.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cccnc3)cc2)C2CC2)CC1 nan
118300921 157295 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 4 5.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccco3)cc2)C2CC2)CC1 nan
CHEMBL3954560 157295 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 4 5.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccco3)cc2)C2CC2)CC1 nan
62706515 83012 0 None -1 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058400 83012 0 None -1 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)OCC3=O)CC1 10.1016/j.bmcl.2012.05.117
89995616 154728 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 479 5 0 6 4.5 COC(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
CHEMBL3933838 154728 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 479 5 0 6 4.5 COC(=O)c1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)cn1 nan
54591953 167556 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 3 1 4 3.7 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL4114216 167556 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 319 3 1 4 3.7 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
68230358 129078 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 461 7 0 7 2.6 CCC(F)(F)C(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598104 129078 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 461 7 0 7 2.6 CCC(F)(F)C(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
25053114 183725 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 522 7 1 12 3.4 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(-c5cccnc5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
CHEMBL462197 183725 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 522 7 1 12 3.4 CS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(-c5cccnc5)no4)CC3)c2[N+](=O)[O-])cc1 10.1021/jm8006867
71654937 97534 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 407 6 1 5 4.7 CCc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.04.014
CHEMBL2391604 97534 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 407 6 1 5 4.7 CCc1ccc(S(=O)(=O)Nc2cccc(Oc3nc(C)cc(C)c3C#N)c2)cc1 10.1016/j.bmcl.2013.04.014
76324299 110006 0 None -5 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 472 6 0 7 3.5 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084372 110006 0 None -5 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 472 6 0 7 3.5 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(F)(F)F)c1C 10.1016/j.bmcl.2011.04.035
54591647 151314 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3907251 151314 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
137660158 165858 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 515 6 0 8 4.6 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)C)CC4)ncnc23)cc1F 10.1016/j.bmcl.2017.06.032
CHEMBL4097314 165858 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 515 6 0 8 4.6 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)C)CC4)ncnc23)cc1F 10.1016/j.bmcl.2017.06.032
71491755 171764 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 460 8 0 4 5.3 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N(C)C3CC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4225589 171764 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 460 8 0 4 5.3 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)N(C)C3CC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
137643239 165079 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 414 8 1 5 3.5 NC(=O)Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1 10.1016/j.bmcl.2017.01.091
CHEMBL4089040 165079 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 414 8 1 5 3.5 NC(=O)Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)cc1 10.1016/j.bmcl.2017.01.091
68211518 117659 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 508 7 0 6 4.4 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ncc(C5CC5)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261128 117659 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 508 7 0 6 4.4 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ncc(C5CC5)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
145959739 168996 0 None -19 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 471 5 1 7 4.9 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4162958 168996 0 None -19 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 471 5 1 7 4.9 CC1(OC(=O)N2[C@H]3CC[C@H]2CC(Oc2ncnc(Nc4ccc(C#N)cc4Cl)c2F)C3)CC1 10.1021/acsmedchemlett.8b00073
67466251 152169 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 411 5 1 5 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(Oc4ccccc4)cc3)oc2c1 nan
CHEMBL3913898 152169 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 411 5 1 5 5.5 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(Oc4ccccc4)cc3)oc2c1 nan
54591104 152028 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 4 1 4 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3912838 152028 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 4 1 4 4.4 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
67464697 155626 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 5 2 6 3.7 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCC4CCNCC4)c3)oc2c1 nan
CHEMBL3941218 155626 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 418 5 2 6 3.7 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCC4CCNCC4)c3)oc2c1 nan
156018872 184708 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 450 5 0 7 4.2 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(S(C)(=O)=O)cc3)cs2)CC1 10.1016/j.bmcl.2019.126855
CHEMBL4645380 184708 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 450 5 0 7 4.2 CC(C)(C)OC(=O)N1CC=C(c2nc(COc3ccc(S(C)(=O)=O)cc3)cs2)CC1 10.1016/j.bmcl.2019.126855
76332225 111797 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 452 4 0 6 3.6 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2021.116208
CHEMBL3113626 111797 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 452 4 0 6 3.6 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2021.116208
71081448 173755 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 548 5 0 6 6.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5cccnc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4287616 173755 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 548 5 0 6 6.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5cccnc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
71655252 97527 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 477 6 1 6 6.1 O=S(=O)(Nc1cccc(Oc2cc(-c3nccs3)cc(Cl)n2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2013.04.014
CHEMBL2391597 97527 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 477 6 1 6 6.1 O=S(=O)(Nc1cccc(Oc2cc(-c3nccs3)cc(Cl)n2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2013.04.014
76332225 111797 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 452 4 0 6 3.6 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113626 111797 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 452 4 0 6 3.6 CC(C)(C)OC(=O)N1CCC(CCOC(=O)N2CCc3cc(S(C)(=O)=O)ccc32)CC1 10.1016/j.bmc.2014.01.028
76331520 110016 0 None -9 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 440 6 0 7 3.3 Cc1c(Oc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084383 110016 0 None -9 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 440 6 0 7 3.3 Cc1c(Oc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
71722055 122943 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358006 122943 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 530 7 0 10 2.9 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
89995528 155462 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 450 5 1 4 4.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(CO)cc3)cc2)C2CC2)CC1 nan
CHEMBL3939845 155462 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 450 5 1 4 4.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(CO)cc3)cc2)C2CC2)CC1 nan
54583893 68355 0 None -17 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 399 4 0 5 3.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771083 68355 0 None -17 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 399 4 0 5 3.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
57402865 77613 0 None -13 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 477 7 1 9 3.3 CCc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951028 77613 0 None -13 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 477 7 1 9 3.3 CCc1c(Nc2ccc(S(C)(=O)=O)nc2C)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
72945709 111405 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 511 6 1 6 5.2 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C1CCCC1)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104894 111405 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 511 6 1 6 5.2 Cc1cc2c(c(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C1CCCC1)C2=O 10.1016/j.bmcl.2013.11.053
155538381 179173 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 459 6 0 6 4.7 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CC(=O)N(C)C)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4476507 179173 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 459 6 0 6 4.7 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(CC(=O)N(C)C)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
54591489 151776 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)(C)N4CCOCC4)cc3)oc2c1 nan
CHEMBL3910893 151776 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)(C)N4CCOCC4)cc3)oc2c1 nan
118711790 120816 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 488 7 0 8 2.9 CCC(F)(F)C(=O)N1CCC(Oc2ncnc(Oc3ccc(S(C)(=O)=O)nc3C)c2F)CC1 10.1016/j.bmcl.2014.06.071
CHEMBL3326681 120816 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 488 7 0 8 2.9 CCC(F)(F)C(=O)N1CCC(Oc2ncnc(Oc3ccc(S(C)(=O)=O)nc3C)c2F)CC1 10.1016/j.bmcl.2014.06.071
118711785 120812 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=S)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326677 120812 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 484 6 0 9 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=S)OC(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
71546200 93012 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 439 5 0 8 3.7 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312509 93012 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 439 5 0 8 3.7 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
51030985 96976 0 None -64 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382414 96976 0 None -64 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
25053254 183638 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 519 8 1 11 4.0 CCS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])c(F)c1 10.1021/jm8006867
CHEMBL461385 183638 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 519 8 1 11 4.0 CCS(=O)(=O)c1ccc(Nc2ncnc(N3CCC(c4nc(C(C)C)no4)CC3)c2[N+](=O)[O-])c(F)c1 10.1021/jm8006867
137655251 165735 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 481 5 0 9 3.2 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4095963 165735 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 481 5 0 9 3.2 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)cc5F)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
68240419 130774 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629481 130774 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 485 4 1 8 4.3 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC(C)(C)C)C2 10.1016/j.bmcl.2015.09.047
68040038 130778 0 None 6 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 499 6 1 9 3.8 COc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629485 130778 0 None 6 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 499 6 1 9 3.8 COc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(C(=O)OC1(C)CC1)C2 10.1016/j.bmcl.2015.09.047
145966749 171158 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 415 8 0 3 6.1 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CC2)CC(C)(C)CCO3)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4213027 171158 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 415 8 0 3 6.1 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@@]3(CC2)CC(C)(C)CCO3)cc1 10.1016/j.bmcl.2018.02.044
76331520 110016 0 None 9 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 440 6 0 7 3.3 Cc1c(Oc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084383 110016 0 None 9 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 440 6 0 7 3.3 Cc1c(Oc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
118722576 122937 0 None 8 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 506 6 0 12 2.3 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2F)cn1 10.1021/jm5011012
CHEMBL3358000 122937 0 None 8 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 506 6 0 12 2.3 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(-n3cnnn3)cc2F)cn1 10.1021/jm5011012
118720414 122670 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 408 4 0 6 3.9 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C#N)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354786 122670 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 408 4 0 6 3.9 COC(=O)C1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C#N)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
73348866 96975 0 None 8 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 492 5 0 8 3.2 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OC2CC(F)(F)C2(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382413 96975 0 None 8 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 492 5 0 8 3.2 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OC2CC(F)(F)C2(F)F)nc1 10.1016/j.bmcl.2013.04.006
70691487 79839 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 476 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
CHEMBL2010845 79839 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 476 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)[C@@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C[C@@H]1F 10.1016/j.bmcl.2011.10.033
155521067 177338 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 492 6 0 7 4.4 C[C@@H](O[C@H]1CC[C@@]2(CC1)CC(F)(F)CO2)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4450117 177338 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 492 6 0 7 4.4 C[C@@H](O[C@H]1CC[C@@]2(CC1)CC(F)(F)CO2)c1nc(-c2cc(F)c(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
89995708 151624 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.6 C[C@H]1CN(C(=O)OC(C)(C)C)CC[C@H]1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
CHEMBL3909707 151624 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.6 C[C@H]1CN(C(=O)OC(C)(C)C)CC[C@H]1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
71116113 130520 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 477 10 0 7 3.6 CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(COC)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
CHEMBL3622177 130520 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 477 10 0 7 3.6 CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(COC)cn3)CC2)c(F)c1 10.1021/acsmedchemlett.5b00207
54586987 68603 0 None 16 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 471 4 0 8 3.4 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773286 68603 0 None 16 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 471 4 0 8 3.4 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
16036825 68007 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1766081 68007 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
53630410 7928 0 None -14 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5739 7928 0 None -14 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1773283 7928 0 None -14 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
11465648 68608 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 474 4 0 10 2.4 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2nnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773291 68608 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 474 4 0 10 2.4 CC(C)(C)OC(=O)N1CCC(Oc2ncnc3c2nnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
54586882 68867 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 7 0 9 3.0 CCCCOC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775172 68867 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 473 7 0 9 3.0 CCCCOC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
46897575 111794 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 484 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2014.01.028
CHEMBL3113623 111794 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 484 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2014.01.028
25053186 183684 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 515 8 1 11 4.2 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(=O)(=O)C(C)C)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL461747 183684 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 515 8 1 11 4.2 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(=O)(=O)C(C)C)cc4)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
25053255 183657 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 533 8 1 11 4.3 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(=O)(=O)C(C)C)cc4F)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
CHEMBL461560 183657 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentationAgonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation
ChEMBL 533 8 1 11 4.3 CC(C)c1noc(C2CCN(c3ncnc(Nc4ccc(S(=O)(=O)C(C)C)cc4F)c3[N+](=O)[O-])CC2)n1 10.1021/jm8006867
86709924 120706 0 None 6 2 Human 8.1 pEC50 = 8.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 5 0 9 3.3 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325844 120706 0 None 6 2 Human 8.1 pEC50 = 8.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 482 5 0 9 3.3 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C)CC2)c1F 10.1016/j.bmcl.2014.06.071
51030711 84200 4 None 23 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
CHEMBL2086690 84200 4 None 23 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assayAgonist activity at human GPR119 transfected in HEK293 cells assessed as cAMP accumulation after 45 mins incubation by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1039/C2MD20130E
68021862 164366 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 475 5 0 7 4.6 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)c(C)cc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4080747 164366 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 475 5 0 7 4.6 CCc1cnc(N2CCC(n3ncc4cc(-c5ccc(S(C)(=O)=O)cc5)c(C)cc43)CC2)nc1 10.1016/j.bmc.2017.06.014
76314040 111700 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 560 6 0 7 6.4 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(F)c(Oc3cc(-c4nnc(C5CC5)o4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112992 111700 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 560 6 0 7 6.4 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(F)c(Oc3cc(-c4nnc(C5CC5)o4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76324934 111726 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 576 6 0 7 6.9 O=S(=O)(c1ccc(Cl)c(Cl)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113018 111726 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 576 6 0 7 6.9 O=S(=O)(c1ccc(Cl)c(Cl)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
68240224 130776 0 None 7 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 520 6 1 9 3.4 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CC2COCC(C1)N2C(=O)OC1(C)CC1 10.1016/j.bmcl.2015.09.047
CHEMBL3629483 130776 0 None 7 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 520 6 1 9 3.4 Cc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CC2COCC(C1)N2C(=O)OC1(C)CC1 10.1016/j.bmcl.2015.09.047
68211918 117668 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 524 8 0 6 4.9 CCCc1cnc(N2CCC(C3(C)Cc4cc(C5=CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261137 117668 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 524 8 0 6 4.9 CCCc1cnc(N2CCC(C3(C)Cc4cc(C5=CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
76320655 110010 0 None -4 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 7 0 7 3.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084377 110010 0 None -4 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 446 7 0 7 3.6 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3S(=O)(=O)CC(C)C)c1C 10.1016/j.bmcl.2011.04.035
67461127 159558 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 425 6 1 5 5.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccccc4)cc3)oc2c1 nan
CHEMBL3973628 159558 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 425 6 1 5 5.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCc4ccccc4)cc3)oc2c1 nan
156013023 184244 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 456 7 0 8 3.8 CCc1cnc(N2CC=C(c3nc(COc4ccc(S(C)(=O)=O)cc4)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
CHEMBL4639029 184244 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 456 7 0 8 3.8 CCc1cnc(N2CC=C(c3nc(COc4ccc(S(C)(=O)=O)cc4)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
24939268 7240 67 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.ejmech.2016.08.023
5653 7240 67 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.ejmech.2016.08.023
CHEMBL461384 7240 67 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.ejmech.2016.08.023
46885170 15190 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 482 9 0 7 3.0 CCCS(=O)(=O)N1CCN(c2ccc(OCCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1093453 15190 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 482 9 0 7 3.0 CCCS(=O)(=O)N1CCN(c2ccc(OCCC3CCN(C(=O)OC(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
57397673 77602 0 None -7 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 385 5 1 7 3.6 Cc1ncccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951015 77602 0 None -7 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 385 5 1 7 3.6 Cc1ncccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
54591797 153853 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 400 4 1 5 4.0 O=C1NN=C(c2ccc3nc(-c4ccc(CN5CCCCC5)cc4)oc3c2)C2CC12 nan
CHEMBL3927202 153853 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 400 4 1 5 4.0 O=C1NN=C(c2ccc3nc(-c4ccc(CN5CCCCC5)cc4)oc3c2)C2CC12 nan
62706854 83082 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1nnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)o1 10.1016/j.bmcl.2012.05.117
CHEMBL2058671 83082 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1nnc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)o1 10.1016/j.bmcl.2012.05.117
66554590 93752 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1021/ml300399u
CHEMBL2323592 93752 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(CO[C@H]2CC[C@H](c3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1021/ml300399u
11677830 77619 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 507 8 1 10 3.5 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1OC(C)C 10.1016/j.bmcl.2011.12.092
CHEMBL1951034 77619 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 507 8 1 10 3.5 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1OC(C)C 10.1016/j.bmcl.2011.12.092
51029782 84189 1 None 26 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 401 5 0 8 2.5 COc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
CHEMBL2086678 84189 1 None 26 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 401 5 0 8 2.5 COc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
89995725 157946 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 461 6 0 6 4.6 COc1ccc(OC(=O)N2CCC(N(C(=O)c3ccc(-c4cnco4)cc3)C3CC3)CC2)cc1 nan
CHEMBL3959648 157946 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 461 6 0 6 4.6 COc1ccc(OC(=O)N2CCC(N(C(=O)c3ccc(-c4cnco4)cc3)C3CC3)CC2)cc1 nan
67449544 129077 0 None -7 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 475 6 0 8 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)Oc4ccccc4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598103 129077 0 None -7 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 475 6 0 8 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)Oc4ccccc4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
54586563 69003 0 None -5 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 448 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778253 69003 0 None -5 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 448 6 0 7 3.1 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(F)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
164618438 191594 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 495 5 0 8 2.2 CC(C)(C)OC(=O)N1CCC(N(c2cc(OC3CN(S(C)(=O)=O)C3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
CHEMBL4851910 191594 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 495 5 0 8 2.2 CC(C)(C)OC(=O)N1CCC(N(c2cc(OC3CN(S(C)(=O)=O)C3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
86566993 173213 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 560 6 0 7 5.7 O=S(=O)(Cc1ccc(-c2ccc3c(c2)CCC2(CCN(c4ncc(Cl)cn4)CC2)O3)cc1)Cc1ccccn1 10.1016/j.bmcl.2018.08.010
CHEMBL4277409 173213 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 560 6 0 7 5.7 O=S(=O)(Cc1ccc(-c2ccc3c(c2)CCC2(CCN(c4ncc(Cl)cn4)CC2)O3)cc1)Cc1ccccn1 10.1016/j.bmcl.2018.08.010
51029603 84187 1 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 371 4 0 7 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086675 84187 1 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 371 4 0 7 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3)cn2)CC1 10.1021/jm300310c
118722572 122932 0 None -7 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 470 5 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2C#N)cn1 10.1021/jm5011012
CHEMBL3357996 122932 0 None -7 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 470 5 0 10 2.9 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C#N)cc2C#N)cn1 10.1021/jm5011012
118711792 120818 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 6 0 8 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3CCCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326683 120818 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 6 0 8 3.1 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3CCCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
56959214 189567 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 7 1 9 4.2 CC(C)COC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4790469 189567 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 7 1 9 4.2 CC(C)COC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
155550456 181049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 438 6 0 7 4.0 CC(O[C@H]1CC[C@]2(CCCO2)CC1)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4549349 181049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 438 6 0 7 4.0 CC(O[C@H]1CC[C@]2(CCCO2)CC1)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
54591572 155176 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 3 2 5 3.3 Cc1cc(=O)[nH]nc1-c1ccc2nc(-c3ccc(C(=O)O)cc3)oc2c1 nan
CHEMBL3937554 155176 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 347 3 2 5 3.3 Cc1cc(=O)[nH]nc1-c1ccc2nc(-c3ccc(C(=O)O)cc3)oc2c1 nan
86694587 141760 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 475 3 0 6 4.2 CC(C)(C)OC(=O)N1CCC(C)(c2cc3cc(C4=CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
CHEMBL3719377 141760 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 475 3 0 6 4.2 CC(C)(C)OC(=O)N1CCC(C)(c2cc3cc(C4=CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
72946092 111391 0 None -4 4 Crab-eating macaque 7.1 pEC50 = 7.1 Functional
Agonist activity at cynomolgus monkey GPR119 assessed as cAMP accumulationAgonist activity at cynomolgus monkey GPR119 assessed as cAMP accumulation
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104879 111391 0 None -4 4 Crab-eating macaque 7.1 pEC50 = 7.1 Functional
Agonist activity at cynomolgus monkey GPR119 assessed as cAMP accumulationAgonist activity at cynomolgus monkey GPR119 assessed as cAMP accumulation
ChEMBL 503 6 1 6 4.8 Cc1cc2c(c(Oc3cc(NS(=O)(=O)c4ccc(Cl)cc4)ccc3F)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
137638017 162769 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 473 6 0 6 4.5 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)(C)C)CC3)cn2)cc1F 10.1016/j.bmcl.2017.06.032
CHEMBL4061666 162769 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 473 6 0 6 4.5 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)(C)C)CC3)cn2)cc1F 10.1016/j.bmcl.2017.06.032
118720421 122677 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 468 4 0 6 4.6 COC(=O)[C@@]1(Cc2cccc(F)c2)N=Cc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354793 122677 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 468 4 0 6 4.6 COC(=O)[C@@]1(Cc2cccc(F)c2)N=Cc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
66964159 117532 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 420 6 0 6 4.5 CCOC(=O)C(C)(Cc1cccnc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260526 117532 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 420 6 0 6 4.5 CCOC(=O)C(C)(Cc1cccnc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
62706852 83080 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1noc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)n1 10.1016/j.bmcl.2012.05.117
CHEMBL2058669 83080 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 384 7 1 7 3.9 CC(C)c1noc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)n1 10.1016/j.bmcl.2012.05.117
54585808 68361 0 None -4 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 413 4 0 5 3.9 Cc1ccc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771090 68361 0 None -4 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 413 4 0 5 3.9 Cc1ccc(N2CCC(C3CCN(c4ccc(S(C)(=O)=O)cc4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
67466191 167664 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)N4CCCCC4)cc3)oc2c1 nan
CHEMBL4115122 167664 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 460 7 1 6 5.0 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC(C)N4CCCCC4)cc3)oc2c1 nan
54591181 158437 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 325 3 1 5 3.8 CCC1CC(c2ccc3nc(-c4cccs4)oc3c2)=NNC1=O nan
CHEMBL3963961 158437 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 325 3 1 5 3.8 CCC1CC(c2ccc3nc(-c4cccs4)oc3c2)=NNC1=O nan
62706692 83018 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)NC3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058406 83018 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)NC3)CC1 10.1016/j.bmcl.2012.05.117
54591183 149228 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 471 7 1 7 4.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCC(C#N)CC4)c3)oc2c1 nan
CHEMBL3890149 149228 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 471 7 1 7 4.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCC(C#N)CC4)c3)oc2c1 nan
62706352 83005 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 409 5 0 5 3.8 CC(C)(C)OC(=O)N1CCC(CCCOc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058394 83005 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 409 5 0 5 3.8 CC(C)(C)OC(=O)N1CCC(CCCOc2ccc3c(c2)CCS3(=O)=O)CC1 10.1016/j.bmcl.2012.05.117
60155100 84168 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
CHEMBL2086655 84168 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ccc(OCc3ccc(S(C)(=O)=O)cc3)nc2)CC1 10.1021/jm300310c
118720410 122666 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 479 4 0 5 5.8 COC(=O)C1(Cc2ccccc2)CCCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354782 122666 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 479 4 0 5 5.8 COC(=O)C1(Cc2ccccc2)CCCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
56643412 79831 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 458 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010836 79831 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 458 6 0 6 3.3 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.10.033
89995514 151829 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 499 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(C)(=O)=O)cn3)cc2)C2CC2)CC1 nan
CHEMBL3911326 151829 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 499 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(S(C)(=O)=O)cn3)cc2)C2CC2)CC1 nan
51354342 68032 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@@H]2[C@H]3CO[C@@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766202 68032 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at GPR119 in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@@H]2[C@H]3CO[C@@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
56959213 188529 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 7 1 9 4.2 CC(C)COC(=O)N1CCC(Oc2cc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4777445 188529 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 498 7 1 9 4.2 CC(C)COC(=O)N1CCC(Oc2cc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)ncn2)CC1 10.1016/j.bmc.2021.116071
53323811 65331 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 396 5 1 3 3.9 CC(CNC(=O)Cc1cccc(F)c1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684031 65331 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 396 5 1 3 3.9 CC(CNC(=O)Cc1cccc(F)c1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
71545538 93032 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 449 4 0 7 4.5 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CCC2)c1C 10.1021/jm301626p
CHEMBL2312528 93032 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 449 4 0 7 4.5 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CCC2)c1C 10.1021/jm301626p
51030811 84188 1 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 385 4 0 7 2.8 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
CHEMBL2086677 84188 1 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 385 4 0 7 2.8 Cc1cnccc1COc1cnc(N2CCN(C(=O)OC(C)(C)C)CC2)nc1 10.1021/jm300310c
68036918 168946 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 447 5 0 7 3.6 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Oc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4162299 168946 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 assessed as increase in cAMP levelAgonist activity at mouse GPR119 assessed as increase in cAMP level
ChEMBL 447 5 0 7 3.6 CC1(OC(=O)N2CC3COCC(C2)C3Oc2ncnc(Oc3ccccc3F)c2F)CC1 10.1021/acsmedchemlett.8b00073
89995533 153066 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 496 6 0 7 4.4 CCOC(=O)c1cnn(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)c1C nan
CHEMBL3920834 153066 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 496 6 0 7 4.4 CCOC(=O)c1cnn(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)c1C nan
68289892 154717 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1ncoc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3933773 154717 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1ncoc1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
56960793 186924 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 512 7 1 9 4.5 Cc1c(Oc2ccc(/C=C3\SC(=O)NC3=O)cc2)ncnc1OC1CCN(C(=O)OCC(C)C)CC1 10.1016/j.bmc.2021.116071
CHEMBL4748865 186924 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 512 7 1 9 4.5 Cc1c(Oc2ccc(/C=C3\SC(=O)NC3=O)cc2)ncnc1OC1CCN(C(=O)OCC(C)C)CC1 10.1016/j.bmc.2021.116071
54591266 152252 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 488 9 1 6 5.6 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCCN5CCCCC5)cc4)oc3c2)[C@H]1C nan
CHEMBL3914488 152252 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 488 9 1 6 5.6 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCCCN5CCCCC5)cc4)oc3c2)[C@H]1C nan
76309731 110002 0 None -204 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL3084368 110002 0 None -204 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 424 6 0 7 4.2 Cc1ncccc1Oc1ncnc(O[C@@H]2C[C@@H]3CC[C@H](C2)N3C(=O)OCC2CC2)c1C 10.1016/j.bmcl.2011.04.035
54584841 68346 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 387 3 1 4 3.6 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(C(N)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771073 68346 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 387 3 1 4 3.6 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccc(C(N)=O)cc3)CC2)CC1 10.1016/j.bmcl.2010.12.086
70693584 79836 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 465 6 0 8 3.1 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2nc3cc(F)ccc3s2)CC1 10.1016/j.bmcl.2011.10.033
CHEMBL2010842 79836 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assayAgonist activity at human GPR119 receptor expressed in HEK293 cells assessed as cAMP accumulation after 45 mins by fluorescence assay
ChEMBL 465 6 0 8 3.1 CN(C(=O)Cc1ccc(-n2cnnn2)cc1)C1CCN(Cc2nc3cc(F)ccc3s2)CC1 10.1016/j.bmcl.2011.10.033
4400062 117515 15 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 457 6 0 5 5.7 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260506 117515 15 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 457 6 0 5 5.7 CCOC(=O)C(Cc1c(F)cccc1Cl)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
70796891 117525 0 None -11 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260518 117525 0 None -11 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 6 0 5 5.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1ccnc2c(-c3ccc(Cl)cc3)cnn12 10.1016/j.bmcl.2014.03.023
73387821 150932 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 436 4 0 5 4.5 Cc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)nn1 nan
CHEMBL3903985 150932 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 436 4 0 5 4.5 Cc1ccc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)nn1 nan
54592035 150491 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 502 7 1 6 6.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4C(C)(C)CCCC4(C)C)cc3)oc2c1 nan
CHEMBL3900433 150491 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 502 7 1 6 6.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4C(C)(C)CCCC4(C)C)cc3)oc2c1 nan
118711789 120599 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 470 6 0 8 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325461 120599 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 470 6 0 8 2.6 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(C)(C)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
118711793 120819 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 464 6 0 8 2.7 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326684 120819 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 464 6 0 8 2.7 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C3(C)CC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
67466360 158952 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 363 3 1 6 3.1 COC(=O)c1ccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)cc1 nan
CHEMBL3968283 158952 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 363 3 1 6 3.1 COC(=O)c1ccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)cc1 nan
137643726 165155 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 479 8 0 7 4.2 CCc1cnc(N2CCC(COc3ccc(-c4ccc(C(=O)N(C)OC)c(F)c4)nc3)CC2)nc1 10.1016/j.bmcl.2017.06.032
CHEMBL4089778 165155 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 479 8 0 7 4.2 CCc1cnc(N2CCC(COc3ccc(-c4ccc(C(=O)N(C)OC)c(F)c4)nc3)CC2)nc1 10.1016/j.bmcl.2017.06.032
118711784 120811 0 None -9 2 Rat 7.1 pEC50 = 7.1 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326676 120811 0 None -9 2 Rat 7.1 pEC50 = 7.1 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
137653591 165682 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 523 6 1 10 3.4 CC(C)(C)OC(=O)N1CC2CC(Oc3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
CHEMBL4095373 165682 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
ChEMBL 523 6 1 10 3.4 CC(C)(C)OC(=O)N1CC2CC(Oc3ncnc(Nc4ccc(S(C)(=O)=O)cc4F)c3[N+](=O)[O-])C1C2 10.1016/j.bmcl.2017.03.092
76332173 111722 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 586 7 0 9 5.0 CS(=O)(=O)c1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
CHEMBL3113014 111722 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 586 7 0 9 5.0 CS(=O)(=O)c1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
62706514 83010 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 400 5 1 4 5.4 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCCCC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058399 83010 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 400 5 1 4 5.4 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCCCC3=O)CC1 10.1016/j.bmcl.2012.05.117
76314096 111804 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 3.9 Cc1c(S(C)(=O)=O)ccc2c1CCN2C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113633 111804 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 3.9 Cc1c(S(C)(=O)=O)ccc2c1CCN2C(=O)OCCC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
67466451 151262 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@H]2CCc3nc(-c4ccccc4)oc3C2)[C@H]2C[C@@H]12 nan
CHEMBL3906777 151262 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C([C@H]2CCc3nc(-c4ccccc4)oc3C2)[C@H]2C[C@@H]12 nan
67466545 152029 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 547 7 1 8 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCN(C(=O)OC(C)(C)C)CC4)c3)oc2c1 nan
CHEMBL3912839 152029 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 547 7 1 8 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN4CCN(C(=O)OC(C)(C)C)CC4)c3)oc2c1 nan
67451300 129081 0 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 437 6 0 7 2.6 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598107 129081 0 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 437 6 0 7 2.6 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
53322450 65332 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 396 5 1 3 3.9 CC(CNC(=O)Cc1cc(F)ccc1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684032 65332 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 396 5 1 3 3.9 CC(CNC(=O)Cc1cc(F)ccc1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
137656947 166481 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 518 5 0 10 3.7 CC(=O)c1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
CHEMBL4104336 166481 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 518 5 0 10 3.7 CC(=O)c1cnc(N2CCC(c3coc4c(N5CCc6cc(S(C)(=O)=O)ccc65)ncnc34)CC2)nc1 10.1016/j.bmcl.2017.06.034
76683814 171790 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 423 7 0 5 4.3 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4225934 171790 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 423 7 0 5 4.3 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2018.02.032
145978767 170532 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 439 9 0 5 5.1 CC(C)(C)OC(=O)N1CCC(CCCCCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
CHEMBL4205488 170532 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 439 9 0 5 5.1 CC(C)(C)OC(=O)N1CCC(CCCCCCOc2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2018.02.044
54589231 117657 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 502 6 0 6 4.2 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ncc(Cl)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
CHEMBL3261126 117657 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 502 6 0 6 4.2 CCCS(=O)(=O)N1CC=C(c2ccc3c(c2)CC(C2CCN(c4ncc(Cl)cn4)CC2)O3)CC1 10.1016/j.bmcl.2014.03.096
68211779 117673 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 540 9 1 7 3.8 CCCc1cnc(N2CCC(C3(C)Cc4cc(C5=CCN(S(=O)(=O)CCCO)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261142 117673 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 540 9 1 7 3.8 CCCc1cnc(N2CCC(C3(C)Cc4cc(C5=CCN(S(=O)(=O)CCCO)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
70688972 84163 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 395 4 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ncc(-c3ccc(OCC#N)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086649 84163 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 395 4 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ncc(-c3ccc(OCC#N)cc3)cn2)CC1 10.1021/jm300310c
60155274 84180 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 469 5 0 8 2.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCC2CCN(S(C)(=O)=O)CC2)cn1 10.1021/jm300310c
CHEMBL2086668 84180 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 469 5 0 8 2.0 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCC2CCN(S(C)(=O)=O)CC2)cn1 10.1021/jm300310c
89995718 151838 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 463 4 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)c(F)c3)cc2)C2CC2)CC1 nan
CHEMBL3911390 151838 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 463 4 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)c(F)c3)cc2)C2CC2)CC1 nan
73388330 158819 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 456 5 0 7 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)c([N+](=O)[O-])c2)C2CC2)CC1 nan
CHEMBL3967234 158819 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 456 5 0 7 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)c([N+](=O)[O-])c2)C2CC2)CC1 nan
145978800 170606 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 9 4.9 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\SC(=O)NC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4206345 170606 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 9 4.9 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\SC(=O)NC5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
71471851 120331 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 472 5 0 7 3.8 CC(C)C(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321832 120331 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 472 5 0 7 3.8 CC(C)C(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
54591648 149800 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@H]1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
CHEMBL3894781 149800 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@H]1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
71736722 140483 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 448 5 0 5 5.0 CC(C)(F)CN1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc3o2)CC1 nan
CHEMBL3715018 140483 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 448 5 0 5 5.0 CC(C)(F)CN1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc3o2)CC1 nan
56592329 166202 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 506 4 1 8 5.1 CC(C)(C)OC(=O)N1CCC(c2csc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL4100997 166202 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 506 4 1 8 5.1 CC(C)(C)OC(=O)N1CCC(c2csc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
73354930 96970 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1CC2CCC(C1)N2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382408 96970 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1CC2CCC(C1)N2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
60155364 84181 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 491 6 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(=O)(=O)N(C)C)cc2)cn1 10.1021/jm300310c
CHEMBL2086669 84181 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 491 6 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(=O)(=O)N(C)C)cc2)cn1 10.1021/jm300310c
89995557 153370 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 513 6 1 5 4.7 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(NS(C)(=O)=O)cc3)cc2)C2CC2)CC1 nan
CHEMBL3923095 153370 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 513 6 1 5 4.7 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(NS(C)(=O)=O)cc3)cc2)C2CC2)CC1 nan
67464507 167150 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@@H]1C nan
CHEMBL4111022 167150 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@@H]1C nan
67464644 167446 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 349 4 1 5 3.8 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)cc3)oc2c1 nan
CHEMBL4113382 167446 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 349 4 1 5 3.8 CC[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC)cc3)oc2c1 nan
58017032 89302 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 502 6 0 10 3.3 CC(C)c1noc(N2CCC(Oc3ncnc4c3CCN4c3ccc(S(C)(=O)=O)cc3F)CC2)n1 10.1021/jm301404a
CHEMBL2177770 89302 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 502 6 0 10 3.3 CC(C)c1noc(N2CCC(Oc3ncnc4c3CCN4c3ccc(S(C)(=O)=O)cc3F)CC2)n1 10.1021/jm301404a
58016984 89315 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 483 5 0 8 4.8 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(-c3nccs3)cc2F)CC1 10.1021/jm301404a
CHEMBL2177783 89315 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 483 5 0 8 4.8 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(-c3nccs3)cc2F)CC1 10.1021/jm301404a
58017011 89826 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 494 5 0 8 3.8 CC(C)OC(=O)N1CCC(Sc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181678 89826 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 494 5 0 8 3.8 CC(C)OC(=O)N1CCC(Sc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
58017036 89836 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 478 6 0 8 3.1 CCCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2181692 89836 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 478 6 0 8 3.1 CCCOC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
56959212 187446 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 470 6 1 9 3.6 CCOC(=O)N1CCC(Oc2cc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4755177 187446 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 470 6 1 9 3.6 CCOC(=O)N1CCC(Oc2cc(Oc3ccc(/C=C4\SC(=O)NC4=O)cc3)ncn2)CC1 10.1016/j.bmc.2021.116071
137634756 162709 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 512 3 0 8 4.8 CC(C)(C)OC(=O)N1CCC(c2coc3c(N4CCCc5cc(S(C)(=O)=O)ccc54)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL4060970 162709 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase incubated for 4 hrs by luciferase reporter gene assay
ChEMBL 512 3 0 8 4.8 CC(C)(C)OC(=O)N1CCC(c2coc3c(N4CCCc5cc(S(C)(=O)=O)ccc54)ncnc23)CC1 10.1016/j.bmcl.2017.06.034
24897885 89307 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 493 5 1 9 2.7 CC(C)OC(=O)N1CCC(Oc2nc(N)nc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
CHEMBL2177775 89307 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 493 5 1 9 2.7 CC(C)OC(=O)N1CCC(Oc2nc(N)nc3c2CCN3c2ccc(S(C)(=O)=O)cc2F)CC1 10.1021/jm301404a
44177592 89830 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 408 4 0 8 2.8 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(C#N)cn2)CC1 10.1021/jm301404a
CHEMBL2181683 89830 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-expressing 6CRE-luciferase gene after 5 hrs by luciferase reporter gene assay
ChEMBL 408 4 0 8 2.8 CC(C)OC(=O)N1CCC(Oc2ncnc3c2CCN3c2ccc(C#N)cn2)CC1 10.1021/jm301404a
25012362 68365 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771094 68365 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)nc1 10.1016/j.bmcl.2010.12.086
76683917 171946 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 446 8 1 4 4.9 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NC3CC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4228249 171946 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 446 8 1 4 4.9 CC(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(C(=O)NC3CC3)c(F)c1)C2 10.1016/j.bmc.2018.02.032
145963524 169101 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 459 5 1 7 4.8 CC(C)OC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
CHEMBL4164666 169101 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 459 5 1 7 4.8 CC(C)OC(=O)N1[C@H]2CC[C@H]1CC(Oc1ncnc(Nc3ccc(C#N)cc3Cl)c1F)C2 10.1021/acsmedchemlett.8b00073
118722582 122944 0 None 13 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
CHEMBL3358007 122944 0 None 13 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
118720409 122665 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 479 5 0 5 5.8 CCOC(=O)[C@@]1(Cc2ccccc2)CCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354781 122665 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 479 5 0 5 5.8 CCOC(=O)[C@@]1(Cc2ccccc2)CCCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
51030711 84200 4 None 23 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2086690 84200 4 None 23 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
51030711 84200 4 None 23 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1021/jm300310c
CHEMBL2086690 84200 4 None 23 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1021/jm300310c
54580747 68166 0 None -1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 434 4 0 6 3.7 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1770161 68166 0 None -1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 434 4 0 6 3.7 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncc(Cl)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
54585809 68363 0 None 1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 467 4 0 5 4.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C(F)(F)F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771092 68363 0 None 1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 467 4 0 5 4.6 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ccc(C(F)(F)F)cn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
66964040 122661 0 None -2 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 487 6 0 5 6.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(Cl)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
CHEMBL3354777 122661 0 None -2 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 487 6 0 5 6.1 CCOC(=O)[C@](C)(Cc1ccccc1)c1c(Cl)cnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.10.010
118720405 122662 0 None -15 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 465 5 0 5 5.4 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354778 122662 0 None -15 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 465 5 0 5 5.4 CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
89995553 159115 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)c(F)c2)C2CC2)CC1 nan
CHEMBL3969850 159115 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 429 4 0 5 4.5 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)c(F)c2)C2CC2)CC1 nan
21897675 68871 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 5 0 9 3.2 CC(C)(C)COC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1775176 68871 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by melanophore assayAgonist activity at human GPR119 by melanophore assay
ChEMBL 487 5 0 9 3.2 CC(C)(C)COC(=O)N1CCC(Oc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2011.03.007
145982637 172590 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 490 4 2 9 4.5 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Nc1ncnc3c(Nc4ccc(C#N)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
CHEMBL4248331 172590 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assayAgonist activity at human GPR119 expressed in CHOK1 cells assessed as cAMP accumulation after 1 hr by ultra LANCE assay
ChEMBL 490 4 2 9 4.5 CC(C)(C)OC(=O)N1[C@H]2CC[C@@H]1C[C@H](Nc1ncnc3c(Nc4ccc(C#N)cc4F)ncnc13)C2 10.1016/j.bmc.2018.06.035
68230201 129065 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 402 4 0 7 3.5 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(C#N)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598092 129065 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 402 4 0 7 3.5 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(C#N)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
76310439 111800 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 466 4 0 6 3.9 CC(COC(=O)N1CCc2cc(S(C)(=O)=O)ccc21)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
CHEMBL3113629 111800 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 466 4 0 6 3.9 CC(COC(=O)N1CCc2cc(S(C)(=O)=O)ccc21)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116208
76310439 111800 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 3.9 CC(COC(=O)N1CCc2cc(S(C)(=O)=O)ccc21)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113629 111800 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 466 4 0 6 3.9 CC(COC(=O)N1CCc2cc(S(C)(=O)=O)ccc21)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2014.01.028
53492528 129056 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598083 129056 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1016/j.bmcl.2015.04.102
118711784 120811 0 None 9 2 Human 8.1 pEC50 = 8.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326676 120811 0 None 9 2 Human 8.1 pEC50 = 8.1 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 496 6 0 9 3.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)SC3CCC3)CC2)c1F 10.1016/j.bmcl.2014.06.071
53491642 129058 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 400 4 0 5 4.7 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(C#N)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598085 129058 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 400 4 0 5 4.7 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(C#N)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
71474456 130506 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 436 7 0 7 3.0 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622164 130506 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells by cAMP assayAgonist activity at human GPR119 expressed in CHO cells by cAMP assay
ChEMBL 436 7 0 7 3.0 CS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1 10.1021/acsmedchemlett.5b00207
156021712 184861 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 464 7 0 10 3.5 CCc1cnc(N2CC=C(c3nc(COc4ccc(-n5cnnn5)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
CHEMBL4647675 184861 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 464 7 0 10 3.5 CCc1cnc(N2CC=C(c3nc(COc4ccc(-n5cnnn5)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2019.126855
71128816 130519 0 None -1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
CHEMBL3622176 130519 0 None -1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 477 9 0 7 3.8 COC(C)c1cnc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)nc1 10.1021/acsmedchemlett.5b00207
51346816 7876 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 416 6 1 3 3.5 O=C(Cc1c(F)ccc(c1F)F)NC[C@H](C1CCN(CC1)C(=O)OC1(C)CC1)F 10.1016/j.bmcl.2011.01.088
5724 7876 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 416 6 1 3 3.5 O=C(Cc1c(F)ccc(c1F)F)NC[C@H](C1CCN(CC1)C(=O)OC1(C)CC1)F 10.1016/j.bmcl.2011.01.088
CHEMBL1683943 7876 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 416 6 1 3 3.5 O=C(Cc1c(F)ccc(c1F)F)NC[C@H](C1CCN(CC1)C(=O)OC1(C)CC1)F 10.1016/j.bmcl.2011.01.088
76321321 111690 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 530 6 0 7 5.9 CCc1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
CHEMBL3112982 111690 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 530 6 0 7 5.9 CCc1noc(-c2cc(Cl)nc(Oc3ccc4c(c3)N(S(=O)(=O)c3ccc(Cl)cc3)CCC4)c2)n1 10.1016/j.bmcl.2013.12.127
76324929 111695 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nnc(C5CC5)o4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112987 111695 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 542 6 0 7 6.3 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2ccc(Oc3cc(-c4nnc(C5CC5)o4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76310375 111699 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 576 6 0 7 6.9 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(Cl)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112991 111699 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 576 6 0 7 6.9 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(Cl)c(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76321323 111701 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 576 6 0 7 6.9 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(Cl)c(Oc3cc(-c4nnc(C5CC5)o4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3112993 111701 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 576 6 0 7 6.9 O=S(=O)(c1ccc(Cl)cc1)N1CCCc2cc(Cl)c(Oc3cc(-c4nnc(C5CC5)o4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76328497 111723 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 522 6 0 7 5.9 Cc1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
CHEMBL3113015 111723 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 522 6 0 7 5.9 Cc1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
58190324 122949 0 None -6 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 548 6 0 9 2.6 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358012 122949 0 None -6 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 548 6 0 9 2.6 C[C@@H]1CN(C(=O)OC2(C(F)(F)F)COC2)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2F)cn1 10.1021/jm5011012
53492463 129083 0 None -1 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 491 7 0 7 3.8 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598109 129083 0 None -1 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 491 7 0 7 3.8 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(C(F)(F)F)CCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
89995562 151018 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 397 6 0 5 4.0 CCCOC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3904656 151018 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 397 6 0 5 4.0 CCCOC(=O)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
67465162 151307 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 419 5 1 6 4.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOCC4)cc3)oc2c1 nan
CHEMBL3907178 151307 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 419 5 1 6 4.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCOCC4)cc3)oc2c1 nan
71462834 89823 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 529 2 1 5 4.5 CC(C)(C)OC(=O)N1CCC2(CCN(C(=O)Nc3ccc(S(C)(=O)=O)cc3Br)CC2)CC1 10.1021/jm301549a
CHEMBL2181673 89823 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 529 2 1 5 4.5 CC(C)(C)OC(=O)N1CCC2(CCN(C(=O)Nc3ccc(S(C)(=O)=O)cc3Br)CC2)CC1 10.1021/jm301549a
46884986 15019 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 481 7 1 6 2.5 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)NC(C)(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1092333 15019 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 481 7 1 6 2.5 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)NC(C)(C)C)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
57397676 77606 0 None -6 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 416 6 0 8 3.7 COc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
CHEMBL1951020 77606 0 None -6 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 416 6 0 8 3.7 COc1ccc(Oc2ncnc(OC3CCN(C(=O)OC(C)C)CC3)c2C)c(C)n1 10.1016/j.bmcl.2011.12.092
56960791 187917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 546 7 1 9 5.1 Cc1c(Oc2ccc(/C=C3\SC(=O)NC3=O)cc2)ncnc1OC1CCN(C(=O)OCc2ccccc2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4760659 187917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 546 7 1 9 5.1 Cc1c(Oc2ccc(/C=C3\SC(=O)NC3=O)cc2)ncnc1OC1CCN(C(=O)OCc2ccccc2)CC1 10.1016/j.bmc.2021.116071
68209532 156998 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4cccnc4)c3)oc2c1 nan
CHEMBL3952155 156998 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 426 6 1 6 4.7 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCc4cccnc4)c3)oc2c1 nan
53318501 65334 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 378 5 1 3 3.8 CC(CNC(=O)Cc1ccccc1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684034 65334 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 378 5 1 3 3.8 CC(CNC(=O)Cc1ccccc1F)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
70688972 84163 0 None -10 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 395 4 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ncc(-c3ccc(OCC#N)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086649 84163 0 None -10 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 395 4 0 7 3.1 CC(C)(C)OC(=O)N1CCN(c2ncc(-c3ccc(OCC#N)cc3)cn2)CC1 10.1021/jm300310c
89995714 156520 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1cc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)ccc1-c1cnco1 nan
CHEMBL3948064 156520 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1cc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)ccc1-c1cnco1 nan
71654938 97535 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 421 6 1 5 5.3 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(C(C)C)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391605 97535 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 421 6 1 5 5.3 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(C(C)C)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
62707005 83083 0 None -6 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 400 7 1 7 4.3 CC(C)c1nsc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)n1 10.1016/j.bmcl.2012.05.117
CHEMBL2058672 83083 0 None -6 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 400 7 1 7 4.3 CC(C)c1nsc(N2CCC(CCCNc3ccc4c(c3)OCC4=O)CC2)n1 10.1016/j.bmcl.2012.05.117
67464651 152120 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C(C2CCc3nc(-c4ccccc4)oc3C2)C2CC12 nan
CHEMBL3913465 152120 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 307 2 1 4 2.6 O=C1NN=C(C2CCc3nc(-c4ccccc4)oc3C2)C2CC12 nan
73388223 151658 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 537 4 0 5 5.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ocnc3I)cc2)C2CC2)CC1 nan
CHEMBL3909975 151658 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 537 4 0 5 5.0 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ocnc3I)cc2)C2CC2)CC1 nan
87223740 190016 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 470 6 1 9 3.6 CCOC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
CHEMBL4796294 190016 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 470 6 1 9 3.6 CCOC(=O)N1CCC(Oc2cc(Oc3cccc(/C=C4\SC(=O)NC4=O)c3)ncn2)CC1 10.1016/j.bmc.2021.116071
71736574 140555 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 464 3 0 7 3.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(N4CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
CHEMBL3715273 140555 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 464 3 0 7 3.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(N4CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
71471638 120329 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 488 5 0 8 4.2 CC(C)OC(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
CHEMBL3321830 120329 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 24 hrs by CRE-luciferase assay
ChEMBL 488 5 0 8 4.2 CC(C)OC(=O)N1CCC(N(C)c2ncnc3c(-c4ccc(S(C)(=O)=O)cc4)csc23)CC1 10.1016/j.bmcl.2014.07.020
145964891 171239 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 583 8 0 8 5.9 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)N(c6ccccc6)C5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
CHEMBL4214024 171239 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 583 8 0 8 5.9 CCc1cnc(N2CCC(c3nc(COc4ccc(/C=C5\CC(=O)N(c6ccccc6)C5=O)cc4F)cs3)CC2)nc1 10.1016/j.bmcl.2017.10.046
54584625 68999 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 453 6 0 8 3.2 CC(C)OC(=O)N1CCC(Oc2cc(Oc3ccc(S(C)(=O)=O)cc3F)ncn2)CC1 10.1016/j.bmcl.2011.04.035
CHEMBL1778140 68999 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 453 6 0 8 3.2 CC(C)OC(=O)N1CCC(Oc2cc(Oc3ccc(S(C)(=O)=O)cc3F)ncn2)CC1 10.1016/j.bmcl.2011.04.035
68211526 117661 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 510 8 0 6 4.5 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
CHEMBL3261130 117661 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 minsAgonist activity at human GPR119 expressed in HEK293 cells co-expressing Flp-In-T-Rex assessed as cAMP accumulation after 60 mins
ChEMBL 510 8 0 6 4.5 CCCc1cnc(N2CCC(C3Cc4cc(C5=CCN(S(=O)(=O)CCC)CC5)ccc4O3)CC2)nc1 10.1016/j.bmcl.2014.03.096
54583895 68366 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
CHEMBL1771095 68366 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 377 3 0 7 2.9 Cc1cnc(N2CCC(C3CCN(c4cc(C#N)nc(C)n4)CC3)CC2)cn1 10.1016/j.bmcl.2010.12.086
76309733 110015 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 449 6 0 6 4.1 Cc1c(Oc2ccccc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084382 110015 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 449 6 0 6 4.1 Cc1c(Oc2ccccc2Cl)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
139437040 182944 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 508 8 0 8 2.3 CC(C)N(C)C(=O)C1CN(c2ncc(N3CC[C@@H](Oc4ccc(OCC(F)(F)F)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
CHEMBL4592996 182944 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 508 8 0 8 2.3 CC(C)N(C)C(=O)C1CN(c2ncc(N3CC[C@@H](Oc4ccc(OCC(F)(F)F)nc4)C3=O)cn2)C1 10.1021/acsmedchemlett.8b00622
54591334 155629 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 403 5 1 5 5.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCCC4)cc3)oc2c1 nan
CHEMBL3941257 155629 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 403 5 1 5 5.1 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OC4CCCC4)cc3)oc2c1 nan
54591717 166792 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL4107942 166792 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 305 2 1 4 3.4 C[C@@H]1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
76320658 110020 0 None -23 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(F)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084387 110020 0 None -23 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 457 6 1 7 3.4 Cc1c(Nc2ccc(F)cc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
137651939 164179 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 573 7 1 8 6.1 CN(c1ncnc2c(-c3ccc(C(=O)NOCc4ccccc4)cc3)csc12)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2017.06.032
CHEMBL4078440 164179 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 573 7 1 8 6.1 CN(c1ncnc2c(-c3ccc(C(=O)NOCc4ccccc4)cc3)csc12)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2017.06.032
137660724 166109 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 484 6 1 8 4.1 CCNC(=O)c1cc(C)c(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(C)c1 10.1016/j.bmc.2017.06.014
CHEMBL4100021 166109 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 484 6 1 8 4.1 CCNC(=O)c1cc(C)c(-c2cc3nnn(C4CCN(c5ncc(CC)cn5)CC4)c3cn2)c(C)c1 10.1016/j.bmc.2017.06.014
71519192 95829 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 470 5 0 8 2.8 CCc1cnc(N2CCC(N3Cc4cn(-c5ccc(S(C)(=O)=O)cc5F)nc4C3)CC2)nc1 10.1016/j.bmcl.2012.10.119
CHEMBL2313412 95829 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 470 5 0 8 2.8 CCc1cnc(N2CCC(N3Cc4cn(-c5ccc(S(C)(=O)=O)cc5F)nc4C3)CC2)nc1 10.1016/j.bmcl.2012.10.119
CHEMBL2364825 95829 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 470 5 0 8 2.8 CCc1cnc(N2CCC(N3Cc4cn(-c5ccc(S(C)(=O)=O)cc5F)nc4C3)CC2)nc1 10.1016/j.bmcl.2012.10.119
16036825 68007 0 None -7 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1766081 68007 0 None -7 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
54591337 166938 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 337 4 1 5 4.0 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccco4)oc3c2)[C@@H]1C nan
CHEMBL4109181 166938 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 337 4 1 5 4.0 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccco4)oc3c2)[C@@H]1C nan
141750309 187036 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 584 8 1 11 2.8 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(c3ncc(-c4ccccc4)o3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
CHEMBL4750433 187036 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assayAgonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
ChEMBL 584 8 1 11 2.8 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(c3ncc(-c4ccccc4)o3)CC1)c(=O)n2C 10.1016/j.ejmech.2019.112017
145967680 171883 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 423 6 0 5 4.3 CC(C)(C)OC(=O)N1CCC2(CC1)CC2CCCOc1ccc(S(C)(=O)=O)cc1 10.1016/j.bmc.2018.02.032
CHEMBL4227271 171883 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 423 6 0 5 4.3 CC(C)(C)OC(=O)N1CCC2(CC1)CC2CCCOc1ccc(S(C)(=O)=O)cc1 10.1016/j.bmc.2018.02.032
54587812 68347 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
CHEMBL1771075 68347 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 345 2 0 4 3.9 CC(C)(C)OC(=O)N1CCC(C2CCN(c3ccccn3)CC2)CC1 10.1016/j.bmcl.2010.12.086
89995641 154654 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 5 3.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3ccnc3)cc2)C2CC2)CC1 nan
CHEMBL3933307 154654 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 410 4 0 5 3.9 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-n3ccnc3)cc2)C2CC2)CC1 nan
67465971 153396 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 453 7 1 5 6.0 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCc5ccccc5)cc4)oc3c2)[C@H]1C nan
CHEMBL3923315 153396 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 453 7 1 5 6.0 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OCc5ccccc5)cc4)oc3c2)[C@H]1C nan
54591723 160152 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 4 1 4 4.1 CCCC1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
CHEMBL3978634 160152 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 4 1 4 4.1 CCCC1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
51029876 84172 0 None -5 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086660 84172 0 None -5 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
73353419 96974 0 None -39 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382412 96974 0 None -39 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
51029876 84172 0 None -5 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086660 84172 0 None -5 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
16036825 68007 0 None -7 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
CHEMBL1766081 68007 0 None -7 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assayAgonist activity at rat GPR119 expressed in human HEK293 cells assessed as increase in cAMP level after 16 hrs by beta-lactamase reporter gene assay
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
118292191 151417 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 445 4 0 4 5.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)cc3)cc2)C2CC2)CC1 nan
CHEMBL3908102 151417 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 445 4 0 4 5.2 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(C#N)cc3)cc2)C2CC2)CC1 nan
67462783 154864 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CC(C)OC(C)C4)cc3)oc2c1 nan
CHEMBL3935045 154864 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 476 7 1 7 4.2 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CC(C)OC(C)C4)cc3)oc2c1 nan
54591485 153740 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 448 9 1 6 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(CC)C(C)C)c3)oc2c1 nan
CHEMBL3926139 153740 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 448 9 1 6 4.9 CCC1CC(=O)NN=C1c1ccc2nc(-c3cccc(OCCN(CC)C(C)C)c3)oc2c1 nan
71654936 97533 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 379 5 1 5 4.2 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccccc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391603 97533 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 379 5 1 5 4.2 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccccc3)c2)n1 10.1016/j.bmcl.2013.04.014
68240486 130773 0 None -3 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 2.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(S(=O)(=O)C1CC1)C2 10.1016/j.bmcl.2015.09.047
CHEMBL3629480 130773 0 None -3 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysisAgonist activity at mouse GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 489 6 1 8 2.9 Cc1c(Nc2ccc(C#N)cc2Cl)ncnc1OC1C2COCC1CN(S(=O)(=O)C1CC1)C2 10.1016/j.bmcl.2015.09.047
67467240 154661 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 6 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCCCN4C)cc3)oc2c1 nan
CHEMBL3933336 154661 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 446 6 1 6 4.6 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCC4CCCCN4C)cc3)oc2c1 nan
155522754 177598 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 425 5 0 8 4.5 CC1(C)C[C@]2(CC[C@H](c3nc(COc4ccc(-n5cnnn5)cc4)cs3)CC2)CO1 10.1016/j.bmcl.2018.12.041
CHEMBL4453416 177598 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 425 5 0 8 4.5 CC1(C)C[C@]2(CC[C@H](c3nc(COc4ccc(-n5cnnn5)cc4)cs3)CC2)CO1 10.1016/j.bmcl.2018.12.041
89995555 155058 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 439 4 0 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3936640 155058 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 439 4 0 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
89995707 167501 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.6 C[C@@H]1CN(C(=O)OC(C)(C)C)CC[C@@H]1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
CHEMBL4113780 167501 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.6 C[C@@H]1CN(C(=O)OC(C)(C)C)CC[C@@H]1N(C(=O)c1ccc(-c2cnco2)cc1)C1CC1 nan
86694582 140653 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 506 4 0 6 4.7 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(c5ccc(C(F)(F)F)cn5)CC4)oc3cn2)CC1 nan
CHEMBL3715651 140653 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 506 4 0 6 4.7 CS(=O)(=O)N1CC=C(c2cc3cc(C4CCN(c5ccc(C(F)(F)F)cn5)CC4)oc3cn2)CC1 nan
76331521 110019 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 439 6 1 7 3.3 Cc1c(Nc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
CHEMBL3084386 110019 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 439 6 1 7 3.3 Cc1c(Nc2ccccc2C#N)ncnc1O[C@@H]1C[C@@H]2CC[C@H](C1)N2S(=O)(=O)C1CC1 10.1016/j.bmcl.2011.04.035
66964459 117541 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 438 5 1 4 5.0 CC(=O)NC(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260537 117541 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 438 5 1 4 5.0 CC(=O)NC(C)(Cc1ccccc1)c1ccnc2c(-c3ccc(C(F)(F)F)cc3)cnn12 10.1016/j.bmcl.2014.03.023
62706513 83009 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058398 83009 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCC3=O)CC1 10.1016/j.bmcl.2012.05.117
155524213 177691 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 452 6 0 7 4.4 CC(O[C@H]1CC[C@]2(CCCCO2)CC1)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4454946 177691 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 452 6 0 7 4.4 CC(O[C@H]1CC[C@]2(CCCCO2)CC1)c1nc(-c2ccc(CS(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
118300925 158434 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 459 5 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(CC#N)cc3)cc2)C2CC2)CC1 nan
CHEMBL3963955 158434 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 459 5 0 4 5.4 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccc(CC#N)cc3)cc2)C2CC2)CC1 nan
76332174 111724 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 544 6 0 7 5.9 O=S(=O)(c1ccc(F)cc1F)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113016 111724 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 544 6 0 7 5.9 O=S(=O)(c1ccc(F)cc1F)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
54583648 68998 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 4 0 7 4.1 Cc1ncccc1Oc1ncnc(O[C@H]2CC3CC2CN3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778137 68998 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 412 4 0 7 4.1 Cc1ncccc1Oc1ncnc(O[C@H]2CC3CC2CN3C(=O)OC(C)(C)C)c1C 10.1016/j.bmcl.2011.04.035
71519190 93119 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 450 4 0 7 2.7 CC(C)OC(=O)N1CCC(N2Cc3cn(-c4ccc(S(C)(=O)=O)cc4F)nc3C2)CC1 10.1016/j.bmcl.2012.10.119
CHEMBL2313411 93119 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells co-expressing CRE beta-lactamase assessed as cAMP accumulation by HTRF assay
ChEMBL 450 4 0 7 2.7 CC(C)OC(=O)N1CCC(N2Cc3cn(-c4ccc(S(C)(=O)=O)cc4F)nc3C2)CC1 10.1016/j.bmcl.2012.10.119
53317211 65340 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 398 6 1 3 3.6 CC1(OC(=O)N2CCC(CCNC(=O)Cc3c(F)ccc(F)c3F)CC2)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1684041 65340 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 398 6 1 3 3.6 CC1(OC(=O)N2CCC(CCNC(=O)Cc3c(F)ccc(F)c3F)CC2)CC1 10.1016/j.bmcl.2011.01.088
54591954 154748 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC(C)C1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3934056 154748 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC(C)C1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
10166 9245 65 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2017.10.046
25025505 9245 65 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2017.10.046
CHEMBL3260505 9245 65 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2017.10.046
DB12345 9245 65 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells co-expressing CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 10.1016/j.bmcl.2017.10.046
58116587 111852 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 459 5 0 7 3.6 CC(C)OC(=O)N1CCC(Oc2ccnc(N3CCc4cc(S(C)(=O)=O)ccc43)c2)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113839 111852 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 459 5 0 7 3.6 CC(C)OC(=O)N1CCC(Oc2ccnc(N3CCc4cc(S(C)(=O)=O)ccc43)c2)CC1 10.1016/j.bmc.2014.01.028
62706513 83009 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCC3=O)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058398 83009 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 372 5 1 4 4.7 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)CCC3=O)CC1 10.1016/j.bmcl.2012.05.117
67462517 152481 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 334 3 2 5 2.8 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(CN)cc3)oc2c1 nan
CHEMBL3916249 152481 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 334 3 2 5 2.8 CC1CC(=O)NN=C1c1ccc2nc(-c3ccc(CN)cc3)oc2c1 nan
54591722 156705 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 4 1 4 4.1 CCCC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3949571 156705 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 4 1 4 4.1 CCCC1CC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
118300920 154279 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 443 4 1 7 3.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3nnc(N)s3)cc2)C2CC2)CC1 nan
CHEMBL3930517 154279 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 443 4 1 7 3.8 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3nnc(N)s3)cc2)C2CC2)CC1 nan
145971825 171333 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 375 8 0 4 4.3 CN(C)C(=O)c1ccc(OCCCCCC2CCC3(CC2)OCCO3)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4215188 171333 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 375 8 0 4 4.3 CN(C)C(=O)c1ccc(OCCCCCC2CCC3(CC2)OCCO3)cc1 10.1016/j.bmcl.2018.02.044
71545535 93029 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.3 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OCC(C)C)c1C 10.1021/jm301626p
CHEMBL2312525 93029 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 437 5 0 7 4.3 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OCC(C)C)c1C 10.1021/jm301626p
62706519 83016 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CO3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058404 83016 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 374 5 1 5 4.1 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)CO3)CC1 10.1016/j.bmcl.2012.05.117
56960507 186269 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 512 5 1 9 4.7 Cc1c(Oc2ccc(/C=C3\SC(=O)NC3=O)cc2)ncnc1OC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116071
CHEMBL4741006 186269 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassayAgonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
ChEMBL 512 5 1 9 4.7 Cc1c(Oc2ccc(/C=C3\SC(=O)NC3=O)cc2)ncnc1OC1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmc.2021.116071
54581118 68604 0 None -25 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 489 4 0 8 3.5 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1 10.1016/j.bmcl.2011.03.007
CHEMBL1773287 68604 0 None -25 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 489 4 0 8 3.5 CC(C)(C)OC(=O)N1CCC(Cc2ncnc3c2cnn3-c2ccc(S(C)(=O)=O)cc2F)CC1 10.1016/j.bmcl.2011.03.007
89995564 160153 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 431 5 0 5 4.6 O=C(Oc1ccccc1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3978636 160153 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 431 5 0 5 4.6 O=C(Oc1ccccc1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
54591408 167266 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 391 5 1 5 4.8 CC[C@H]1C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)=NNC(=O)[C@@H]1C nan
CHEMBL4111982 167266 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 391 5 1 5 4.8 CC[C@H]1C(c2ccc3nc(-c4ccc(OC(C)C)cc4)oc3c2)=NNC(=O)[C@@H]1C nan
67464967 167561 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 4.8 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cc(C)cs4)oc3c2)[C@@H]1C nan
CHEMBL4114273 167561 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 367 4 1 5 4.8 CCC[C@H]1C(=O)NN=C(c2ccc3nc(-c4cc(C)cs4)oc3c2)[C@@H]1C nan
66964035 117518 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 7 0 8 4.0 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3nc(C(C)C)no3)cnn12 10.1016/j.bmcl.2014.03.023
CHEMBL3260509 117518 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 419 7 0 8 4.0 CCOC(=O)C(C)(Cc1ccccc1)c1ccnc2c(-c3nc(C(C)C)no3)cnn12 10.1016/j.bmcl.2014.03.023
118711787 120814 0 None -5 2 Rat 6.1 pEC50 = 6.1 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 5 0 8 2.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326679 120814 0 None -5 2 Rat 6.1 pEC50 = 6.1 Functional
Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 478 5 0 8 2.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
58116595 111855 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2ccnc(N3CCc4cc(S(C)(=O)=O)ccc43)n2)CC1 10.1016/j.bmc.2014.01.028
CHEMBL3113841 111855 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 transfected in CHO cells assessed as cAMP accumulation after 2 hrs by luciferase reporter gene assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2ccnc(N3CCc4cc(S(C)(=O)=O)ccc43)n2)CC1 10.1016/j.bmc.2014.01.028
53318456 65321 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 438 6 1 5 3.0 CC(CNC(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
CHEMBL1683945 65321 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assayAgonist activity against human GPR119 receptor expressed in HEK293 cells assessed as beta-lactamase production by cAMP response element assay
ChEMBL 438 6 1 5 3.0 CC(CNC(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2011.01.088
73388224 158577 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)co1 nan
CHEMBL3965125 158577 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 425 4 0 5 4.7 Cc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)co1 nan
67464878 155911 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@H]1C nan
CHEMBL3943319 155911 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 333 3 1 4 4.0 CC[C@H]1C(c2ccc3nc(-c4ccccc4)oc3c2)=NNC(=O)[C@H]1C nan
89995527 149650 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 485 5 1 7 4.2 CC(=O)Nc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)ns1 nan
CHEMBL3893450 149650 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 485 5 1 7 4.2 CC(=O)Nc1nc(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)ns1 nan
25012522 68357 0 None -9 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771085 68357 0 None -9 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
71655253 97528 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 505 7 1 6 6.7 CCc1csc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391598 97528 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 505 7 1 6 6.7 CCc1csc(-c2cc(Cl)nc(Oc3cccc(NS(=O)(=O)c4ccc(Cl)cc4)c3)c2)n1 10.1016/j.bmcl.2013.04.014
155532657 178561 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 452 5 0 7 4.5 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(S(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2018.12.041
CHEMBL4467856 178561 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 452 5 0 7 4.5 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(S(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2018.12.041
51030987 84201 0 None -6 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2noc(C3CC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2086691 84201 0 None -6 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 418 6 0 10 2.3 C[C@@H]1CN(c2noc(C3CC3)n2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
67450949 129061 0 None -8 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 454 6 0 7 3.5 Cc1nc(S(C)(=O)=O)ccc1O[C@H]1CC[C@H](OC2CCN(C(=O)OC(C)C)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598088 129061 0 None -8 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 454 6 0 7 3.5 Cc1nc(S(C)(=O)=O)ccc1O[C@H]1CC[C@H](OC2CCN(C(=O)OC(C)C)CC2)CC1 10.1016/j.bmcl.2015.04.102
155532657 178561 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 452 5 0 7 4.5 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(S(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
CHEMBL4467856 178561 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 minsAgonist activity at recombinant human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation measured after 30 mins
ChEMBL 452 5 0 7 4.5 CC(O[C@H]1CC[C@]2(CC1)COC(C)(C)C2)c1nc(-c2ccc(S(C)(=O)=O)c(F)c2)no1 10.1016/j.bmcl.2019.07.004
89995722 154501 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 449 5 0 5 4.7 O=C(Oc1ccc(F)cc1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
CHEMBL3932134 154501 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 449 5 0 5 4.7 O=C(Oc1ccc(F)cc1)N1CCC(N(C(=O)c2ccc(-c3cnco3)cc2)C2CC2)CC1 nan
67467158 151634 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 2 5 3.1 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(O)c3)oc2c1 nan
CHEMBL3909767 151634 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 321 2 2 5 3.1 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(O)c3)oc2c1 nan
62706692 83018 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)NC3)CC1 10.1016/j.bmcl.2012.05.117
CHEMBL2058406 83018 0 None -1 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse GPR119 receptor expressed in CHO-K1 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 373 5 2 4 3.8 CC(C)(C)OC(=O)N1CCC(CCCNc2ccc3c(c2)C(=O)NC3)CC1 10.1016/j.bmcl.2012.05.117
54591721 154442 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 331 4 1 4 3.9 C=CCC1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
CHEMBL3931714 154442 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 331 4 1 4 3.9 C=CCC1CC(c2ccc3nc(-c4ccccc4)oc3c2)=NNC1=O nan
60155184 84170 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
CHEMBL2086658 84170 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 receptor over expressed in HEK293S cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 447 5 0 7 3.6 CC(C)(C)OC(=O)N1CCC(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1021/jm300310c
67464836 158601 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 361 3 1 6 3.3 COC(=O)c1cccc(-c2nc3ccc(-c4n[nH]c(=O)cc4C)cc3o2)c1 nan
CHEMBL3965335 158601 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 361 3 1 6 3.3 COC(=O)c1cccc(-c2nc3ccc(-c4n[nH]c(=O)cc4C)cc3o2)c1 nan
67466755 159073 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 345 4 1 4 4.2 C=CC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
CHEMBL3969440 159073 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 345 4 1 4 4.2 C=CC[C@H]1C(=O)NN=C(c2ccc3nc(-c4ccccc4)oc3c2)[C@H]1C nan
71736241 141181 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 461 3 0 6 4.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(C4=CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
CHEMBL3717448 141181 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 461 3 0 6 4.0 CC(C)(C)OC(=O)N1CCC(c2cc3cc(C4=CCN(S(C)(=O)=O)CC4)ncc3o2)CC1 nan
67973596 141704 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 474 3 0 6 5.2 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc3o2)CC1 nan
CHEMBL3719203 141704 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assayActivation of human GPR119 expressed in mouse MIN6 cells incubated for 45 mins assessed as stimulation of intracellular cAMP accumulation by AlphaScreen cAMP assay
ChEMBL 474 3 0 6 5.2 CC(C)(C)OC(=O)N1CCC(c2cc3cc(-c4ccc(S(C)(=O)=O)cc4F)ncc3o2)CC1 nan
54581962 68370 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771099 68370 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 458 8 1 5 4.5 O=C(NC1CC1)c1ccc(OCC2CC2CC2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
76683709 171733 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 455 6 0 5 4.8 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
CHEMBL4225084 171733 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by HTRF assay
ChEMBL 455 6 0 5 4.8 CC(C)(C)OC(=O)N1CCC2(CC1)CC(CCCOc1ccc(S(C)(=O)=O)c(F)c1)C2 10.1016/j.bmc.2018.02.032
137632950 163362 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 481 5 0 9 3.2 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)c(F)c5)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
CHEMBL4068645 163362 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay
ChEMBL 481 5 0 9 3.2 CCc1cnc(N2CCC(n3nnc4cc(-c5ccc(S(C)(=O)=O)c(F)c5)ncc43)CC2)nc1 10.1016/j.bmc.2017.06.014
72945900 111393 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 499 6 1 6 4.9 Cc1cc2c(c(Oc3ccc(C)c(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
CHEMBL3104881 111393 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 499 6 1 6 4.9 Cc1cc2c(c(Oc3ccc(C)c(NS(=O)(=O)c4ccc(Cl)cc4)c3)n1)C(=O)N(C(C)C)C2=O 10.1016/j.bmcl.2013.11.053
73353420 96977 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382415 96977 0 None 5 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assayAgonist activity at human GPR119 overexpressed in HEK293S cells assessed as change in cAMP level after 45 mins by HTRF assay
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
54583896 68368 0 None 1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
CHEMBL1771097 68368 0 None 1 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 444 7 1 5 4.1 O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F 10.1016/j.bmcl.2010.12.086
118720408 122664 0 None -2 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 469 4 0 5 5.2 COC(=O)[C@@]1(Cc2cccc(F)c2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
CHEMBL3354780 122664 0 None -2 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF methodAgonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
ChEMBL 469 4 0 5 5.2 COC(=O)[C@@]1(Cc2cccc(F)c2)CCc2cnc3c(-c4ccc(C(F)(F)F)cc4)cnn3c21 10.1016/j.bmcl.2014.10.010
89995651 159234 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 447 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2cc(F)c(-c3cnco3)c(F)c2)C2CC2)CC1 nan
CHEMBL3970904 159234 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 447 4 0 5 4.6 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2cc(F)c(-c3cnco3)c(F)c2)C2CC2)CC1 nan
122184148 129087 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
CHEMBL3598113 129087 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
118711219 120714 0 None 12 2 Human 8.0 pEC50 = 8.0 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325852 120714 0 None 12 2 Human 8.0 pEC50 = 8.0 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
89583933 164400 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 455 8 0 6 3.6 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1)N1CCC1 10.1016/j.bmcl.2017.01.091
CHEMBL4081159 164400 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay
ChEMBL 455 8 0 6 3.6 O=C(Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(c3ncc(Cl)cn3)CC2)nc1)N1CCC1 10.1016/j.bmcl.2017.01.091
67449544 129077 0 None 7 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 475 6 0 8 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)Oc4ccccc4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598103 129077 0 None 7 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 by HTRF cAMP assayAgonist activity at human GPR119 by HTRF cAMP assay
ChEMBL 475 6 0 8 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)Oc4ccccc4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
11503692 77598 0 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
CHEMBL1951011 77598 0 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1016/j.bmcl.2011.12.092
11282871 7870 0 None -8 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
5737 7870 0 None -8 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
CHEMBL1775169 7870 0 None -8 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat GPR119 by melanophore assayAgonist activity at rat GPR119 by melanophore assay
ChEMBL 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 10.1016/j.bmcl.2011.03.007
118711775 120800 0 None 11 2 Human 8.0 pEC50 = 8.0 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3326666 120800 0 None 11 2 Human 8.0 pEC50 = 8.0 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 522 6 0 9 3.4 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)O[C@@H](C)C(F)(F)F)CC2)c1F 10.1016/j.bmcl.2014.06.071
90115611 130509 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 451 8 0 7 3.8 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
CHEMBL3622167 130509 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse GPR119 by cAMP assayAgonist activity at mouse GPR119 by cAMP assay
ChEMBL 451 8 0 7 3.8 CC(C)c1noc(N2CCC([C@H]3C[C@H]3COCc3ccc(S(C)(=O)=O)cc3F)CC2)n1 10.1021/acsmedchemlett.5b00207
76324933 111720 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 526 6 0 7 5.7 O=S(=O)(c1ccc(F)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113012 111720 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 526 6 0 7 5.7 O=S(=O)(c1ccc(F)cc1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
76332172 111721 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 538 7 0 8 5.6 COc1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
CHEMBL3113013 111721 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 538 7 0 8 5.6 COc1ccc(S(=O)(=O)N2CCCc3ccc(Oc4cc(-c5nc(C6CC6)no5)cc(Cl)n4)cc32)cc1 10.1016/j.bmcl.2013.12.127
76314048 111725 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 544 6 0 7 5.9 O=S(=O)(c1ccc(F)c(F)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
CHEMBL3113017 111725 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 544 6 0 7 5.9 O=S(=O)(c1ccc(F)c(F)c1)N1CCCc2ccc(Oc3cc(-c4nc(C5CC5)no4)cc(Cl)n3)cc21 10.1016/j.bmcl.2013.12.127
46865202 14641 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 522 8 0 7 3.8 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)CC4CCCCC4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1089857 14641 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 522 8 0 7 3.8 CC(C)OC(=O)N1CCC(COc2ccc(N3CCN(S(=O)(=O)CC4CCCCC4)CC3)nc2)CC1 10.1016/j.bmcl.2010.02.083
46885050 14635 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 543 9 1 6 4.4 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)Nc4ccc(C(C)C)cc4)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
CHEMBL1089839 14635 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assayAgonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay
ChEMBL 543 9 1 6 4.4 CCCS(=O)(=O)N1CCN(c2ccc(OCC3CCN(C(=O)Nc4ccc(C(C)C)cc4)CC3)cn2)CC1 10.1016/j.bmcl.2010.02.083
90656488 117514 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 456 7 0 8 4.0 CC(C)c1noc(N2CCC(COc3ccc(-c4ccc(S(C)(=O)=O)nc4)cc3)CC2)n1 10.1016/j.bmcl.2014.03.023
CHEMBL3260504 117514 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assayAgonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
ChEMBL 456 7 0 8 4.0 CC(C)c1noc(N2CCC(COc3ccc(-c4ccc(S(C)(=O)=O)nc4)cc3)CC2)n1 10.1016/j.bmcl.2014.03.023
67462520 150843 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 330 2 1 5 3.2 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(C#N)c3)oc2c1 nan
CHEMBL3903213 150843 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 330 2 1 5 3.2 CC1CC(=O)NN=C1c1ccc2nc(-c3cccc(C#N)c3)oc2c1 nan
71655251 97526 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 461 6 1 6 5.6 O=S(=O)(Nc1cccc(Oc2cc(-c3ncco3)cc(Cl)n2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2013.04.014
CHEMBL2391596 97526 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 461 6 1 6 5.6 O=S(=O)(Nc1cccc(Oc2cc(-c3ncco3)cc(Cl)n2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2013.04.014
118722583 122945 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 7 1 10 3.5 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=N)=O)cc2F)cn1 10.1021/jm5011012
CHEMBL3358008 122945 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 529 7 1 10 3.5 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccc(CS(C)(=N)=O)cc2F)cn1 10.1021/jm5011012
51030898 84235 0 None -9 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1noc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)n1 10.1021/jm300310c
CHEMBL2087084 84235 0 None -9 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 420 6 0 10 2.5 CC(C)c1noc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)n1 10.1021/jm300310c
51030897 84237 0 None -18 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
CHEMBL2087086 84237 0 None -18 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 446 5 0 10 2.4 C[C@@H]1CN(c2nc(C(F)(F)F)no2)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1021/jm300310c
67466762 158847 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 489 7 1 7 3.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(C)=O)CC4)cc3)oc2c1 nan
CHEMBL3967399 158847 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 489 7 1 7 3.3 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCN(C(C)=O)CC4)cc3)oc2c1 nan
54586564 69004 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 444 6 0 8 2.3 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(=O)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
CHEMBL1778254 69004 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cMAP level by cell-based cAMP assay
ChEMBL 444 6 0 8 2.3 Cc1ncccc1Oc1ncnc(O[C@H]2C[C@@H]3CC(=O)[C@@H](C2)N3S(=O)(=O)C2CC2)c1C 10.1016/j.bmcl.2011.04.035
137639995 163511 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 459 7 0 6 4.2 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)cc1F 10.1016/j.bmcl.2017.06.032
CHEMBL4070332 163511 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 459 7 0 6 4.2 CON(C)C(=O)c1ccc(-c2ccc(OCC3CCN(C(=O)OC(C)C)CC3)cn2)cc1F 10.1016/j.bmcl.2017.06.032
127048494 147808 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 487 6 2 7 3.3 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4cc(F)c(C(=O)NCCO)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3823972 147808 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 487 6 2 7 3.3 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4cc(F)c(C(=O)NCCO)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
57397673 77602 0 None 7 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 385 5 1 7 3.6 Cc1ncccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951015 77602 0 None 7 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at human GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 385 5 1 7 3.6 Cc1ncccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
67462504 149352 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.4 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OC)cc4)oc3c2)[C@H]1C nan
CHEMBL3891099 149352 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 377 5 1 5 4.4 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(OC)cc4)oc3c2)[C@H]1C nan
118711214 120709 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 493 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C#N)CC2)c1F 10.1016/j.bmcl.2014.06.071
CHEMBL3325847 120709 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assayInhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
ChEMBL 493 6 0 10 2.8 Cc1nc(S(C)(=O)=O)ccc1Oc1ncnc(OC2CCN(C(=O)OC(C)(C)C#N)CC2)c1F 10.1016/j.bmcl.2014.06.071
23649212 77608 2 None -6 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
CHEMBL1951022 77608 2 None -6 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assayAgonist activity at rat GPR119 receptor assessed as cAMP production by HTRF assay
ChEMBL 463 6 1 9 3.0 Cc1nc(S(C)(=O)=O)ccc1Nc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1016/j.bmcl.2011.12.092
122184146 129085 0 None -3 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 455 7 0 7 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598111 129085 0 None -3 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 455 7 0 7 3.3 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(CC4(F)CCCC4)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
118300913 160661 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 438 4 0 5 4.5 Cc1cn(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)c(C)n1 nan
CHEMBL3983016 160661 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 438 4 0 5 4.5 Cc1cn(-c2ccc(C(=O)N(C3CC3)C3CCN(C(=O)OC(C)(C)C)CC3)cc2)c(C)n1 nan
71459320 89266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 420 2 1 6 3.3 CC(C)(C)OC(=O)N1CCC2(CC1)CC(C(=O)Nc1cc(F)c(C#N)cc1F)=NO2 10.1021/jm301549a
CHEMBL2177150 89266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assayAgonist activity at human GPR119 expressed in MIN6 cells assessed as intracellular cAMP level after 45 mins by ALPHAscreen cAMP assay
ChEMBL 420 2 1 6 3.3 CC(C)(C)OC(=O)N1CCC2(CC1)CC(C(=O)Nc1cc(F)c(C#N)cc1F)=NO2 10.1021/jm301549a
2661 9630 65 None -4 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2019.126855
5283454 9630 65 None -4 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2019.126855
CHEMBL280065 9630 65 None -4 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assayAgonist activity at GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1016/j.bmcl.2019.126855
67462394 149308 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 309 2 1 5 3.6 Cc1cc(=O)[nH]nc1-c1ccc2nc(-c3cccs3)oc2c1 nan
CHEMBL3890791 149308 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 309 2 1 5 3.6 Cc1cc(=O)[nH]nc1-c1ccc2nc(-c3cccs3)oc2c1 nan
17993480 154466 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 313 2 2 6 1.1 CC1CC(=O)NN=C1c1ccc2nc(N3CCNCC3)oc2c1 nan
CHEMBL3931876 154466 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 313 2 2 6 1.1 CC1CC(=O)NN=C1c1ccc2nc(N3CCNCC3)oc2c1 nan
58190405 84171 0 None -2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
CHEMBL2086659 84171 0 None -2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at mouse GPR119 receptor assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 462 5 0 8 2.9 C[C@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1021/jm300310c
53492467 129054 0 None -5 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598081 129054 0 None -5 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 453 5 0 6 4.2 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
54590929 155733 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 1 5 3.4 COc1ccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)cc1 nan
CHEMBL3942032 155733 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 335 3 1 5 3.4 COc1ccc(-c2nc3ccc(C4=NNC(=O)CC4C)cc3o2)cc1 nan
145974170 170312 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 373 8 0 3 5.1 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
CHEMBL4202826 170312 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 373 8 0 3 5.1 CN(C)C(=O)c1ccc(OCCCCC[C@H]2CC[C@]3(CCCO3)CC2)cc1 10.1016/j.bmcl.2018.02.044
134151859 159940 3 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 560 8 2 10 1.6 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(C(=O)Nc3ccccc3)CC1)c(=O)n2C 10.1016/j.ejmech.2016.08.023
CHEMBL3976778 159940 3 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 560 8 2 10 1.6 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(CCCN1CCC(C(=O)Nc3ccccc3)CC1)c(=O)n2C 10.1016/j.ejmech.2016.08.023
71716097 92963 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 507 4 0 9 4.4 Cc1c(Oc2ccc(-n3cncn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312161 92963 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assayAgonist activity at human GPR119 in HEK293 cells assessed as cAMP accumulation after 30 mins by CRE-beta-lactamase reporter gene assay
ChEMBL 507 4 0 9 4.4 Cc1c(Oc2ccc(-n3cncn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
89995539 157573 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 0 5 5.9 Cc1nc(-c2ccccc2)cn1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
CHEMBL3956696 157573 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 500 5 0 5 5.9 Cc1nc(-c2ccccc2)cn1-c1ccc(C(=O)N(C2CC2)C2CCN(C(=O)OC(C)(C)C)CC2)cc1 nan
164609814 191996 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 509 6 0 8 2.5 CC(C)(C)OC(=O)N1CCC(N(c2cc(OCC3CN(S(C)(=O)=O)C3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
CHEMBL4857801 191996 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 509 6 0 8 2.5 CC(C)(C)OC(=O)N1CCC(N(c2cc(OCC3CN(S(C)(=O)=O)C3)ncn2)C(F)(F)F)CC1 10.1016/j.bmc.2021.116208
71655012 97538 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 404 5 1 6 4.0 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(C#N)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
CHEMBL2391608 97538 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 minsAgonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 30 mins
ChEMBL 404 5 1 6 4.0 Cc1cc(C)c(C#N)c(Oc2cccc(NS(=O)(=O)c3ccc(C#N)cc3)c2)n1 10.1016/j.bmcl.2013.04.014
136088925 149281 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 363 4 2 5 4.1 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(O)cc4)oc3c2)[C@H]1C nan
CHEMBL3890570 149281 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 363 4 2 5 4.1 CCC[C@@H]1C(=O)NN=C(c2ccc3nc(-c4ccc(O)cc4)oc3c2)[C@H]1C nan
54591021 152677 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 297 2 1 5 3.2 O=C1CCC(c2ccc3nc(-c4cccs4)oc3c2)=NN1 nan
CHEMBL3917764 152677 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 297 2 1 5 3.2 O=C1CCC(c2ccc3nc(-c4cccs4)oc3c2)=NN1 nan
68022271 147700 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 425 4 1 6 3.5 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(C(N)=O)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
CHEMBL3822567 147700 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assayAgonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells after 30 mins by cAMP accumulation assay
ChEMBL 425 4 1 6 3.5 CC(C)OC(=O)N1CCC(n2ncc3cc(-c4ccc(C(N)=O)cc4F)ncc32)CC1 10.1016/j.bmcl.2016.06.050
145949889 169597 0 None -229 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 536 7 1 10 3.1 COc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1C[C@@H]2COC[C@@H](C1)N2C(=O)OC1(C)CC1 10.1021/acsmedchemlett.8b00073
CHEMBL4172551 169597 0 None -229 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by LANCE assay
ChEMBL 536 7 1 10 3.1 COc1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1C[C@@H]2COC[C@@H](C1)N2C(=O)OC1(C)CC1 10.1021/acsmedchemlett.8b00073
67464442 156450 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 471 7 1 7 4.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC(C#N)CC4)cc3)oc2c1 nan
CHEMBL3947531 156450 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 471 7 1 7 4.4 CCC1CC(=O)NN=C1c1ccc2nc(-c3ccc(OCCN4CCC(C#N)CC4)cc3)oc2c1 nan
122184147 129086 0 None -3 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
CHEMBL3598112 129086 0 None -3 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat GPR119 by HTRF cAMP assayAgonist activity at rat GPR119 by HTRF cAMP assay
ChEMBL 479 8 0 10 2.8 CC(C)c1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
118722579 122940 0 None -16 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
CHEMBL3358003 122940 0 None -16 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at mouse GPR119 expressed in HEK293S cells assessed as cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 514 7 0 9 3.2 C[C@@H]1CN(c2nnc(C(F)(F)F)o2)CCN1c1ncc(OCc2ccc(C[S+](C)[O-])cc2F)cn1 10.1021/jm5011012
25012522 68357 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
CHEMBL1771085 68357 0 None 9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assayAgonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 4 0 6 3.0 CS(=O)(=O)c1ccc(N2CCC(C3CCN(c4ncccn4)CC3)CC2)cc1 10.1016/j.bmcl.2010.12.086
71081449 173340 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 548 5 0 6 6.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccncc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
CHEMBL4279705 173340 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assayAgonist activity at human GPR119 expressed in CHO-K1 cells after 4 hrs by Bright-Glo luciferase assay
ChEMBL 548 5 0 6 6.0 CC(C)(C)OC(=O)N1CCC2(CCc3cc(-c4ccc(CS(=O)(=O)Cc5ccncc5)cc4)ccc3O2)CC1 10.1016/j.bmcl.2018.08.010
137632493 163265 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 511 5 0 8 4.8 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1 10.1016/j.bmcl.2017.06.032
CHEMBL4067537 163265 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at human GPR119 expressed in CHOK1 cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 511 5 0 8 4.8 CON(C)C(=O)c1ccc(-c2csc3c(N(C)C4CCN(C(=O)OC(C)(C)C)CC4)ncnc23)cc1 10.1016/j.bmcl.2017.06.032
155515632 176767 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 491 6 1 7 5.4 CC(C)c1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
CHEMBL4442128 176767 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GPR119 expressed in HEK293 cells assessed as intracellular cAMP accumulation after 30 mins by HTRF assay
ChEMBL 491 6 1 7 5.4 CC(C)c1c(Nc2ccc(S(C)(=O)=O)cc2F)ncnc1O[C@H]1CC[C@]2(CC1)COC(C)(C)C2 10.1016/j.bmcl.2018.12.041
67466692 151494 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 320 3 2 4 3.3 CCC1NC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
CHEMBL3908729 151494 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] were stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP-848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM beta-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37 C. 5% CO2. For the assay, the cells are placed in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37 C./5% CO2.After the medium has been sucked out of the wells completely, 10 ul of the test compound are added, the compounds are diluted beforehand with stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes' incubation at RT, the cAMP concentrations are determined using the AlphaScreen cAMP Assay.
ChEMBL 320 3 2 4 3.3 CCC1NC(=O)NN=C1c1ccc2nc(-c3ccccc3)oc2c1 nan
90001549 149726 0 None - 1 Human 7.0 pEC50 = 7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 5 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccno3)cc2)C2CC2)CC1 nan
CHEMBL3894142 149726 0 None - 1 Human 7.0 pEC50 = 7 Functional
AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).AlphaScreen cAMP Assay: MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. No. NP_848566). Min-6/hGPR119 cells are cultured in DMEM, 10% FBS, 50 uM β-mercaptoethanol, 0.3 mg/mL Geniticin, 2 mM GlutaMAX at 37° C. 5% CO2. For the assay, the cells are seeded in Optiplates (white, 384-well, 160W-barcoded, TC, sterile with lid, Cat. No. #6007688 (Perkin Elmer); 10000 cells/well; 50 ul). The plates covered with lids are then incubated for 24 hours at 37° C./5% CO2. After the medium is aspirated from the wells completely, 10 ul of the test compound are added, the compounds are diluted using stimulating buffer (140 mM NaCl, 3.6 mM KCl, 0.5 mM NaH2PO4, 0.5 mM MgSO4, 1.5 mM CaCl2, 10 mM Hepes, 5 mM NaHCO3; pH 7.4. 0.5 mM IBMX and 0.1% BSA, the final DMSO concentration is 1%). After 45 minutes incubation at room temperature (approx. 20° C.), the cAMP concentrations are determined using the AlphaScreen cAMP Assay Kit (Cat. No. #6760625R from PerkinElmer). 10 ul of Biotin-cAMP (final concentration 1 U/well in lysing buffer (5 mM Hepes (pH 7.4), 0.1% BSA, 0.5% Tween) and 10 uL Bead solution (final concentration 1 U/well in lysing buffer) are added. The plates are incubated for another 2 hours at room temperature. The cAMP concentrations are calculated using a cAMP standard curve from the Alpha Screen Counts. The data analysis is carried out by calculating the EC50 value and the maximum value based on a positive control, using suitable software (Graphpad Prism).
ChEMBL 411 4 0 5 4.3 CC(C)(C)OC(=O)N1CCC(N(C(=O)c2ccc(-c3ccno3)cc2)C2CC2)CC1 nan
10049468 193221 7 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayInverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 450 6 0 8 3.7 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(Br)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL487639 193221 7 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayInverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 450 6 0 8 3.7 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(Br)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
25052969 195755 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayInverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 446 10 0 10 3.0 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(OCCOC)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL508439 195755 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayInverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 446 10 0 10 3.0 CCOC(=O)C1CCN(c2ncnc(Oc3ccc(OCCOC)cc3)c2[N+](=O)[O-])CC1 10.1021/jm8006867
3766553 183685 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayInverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 444 6 0 10 2.7 CCOC(=O)C1CCN(c2ncnc(Oc3cc(C(F)(F)F)nn3C)c2[N+](=O)[O-])CC1 10.1021/jm8006867
CHEMBL461765 183685 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assayInverse agonist activity at GPR119 expressed in HEK293 cells assessed as cAMP level by flash plate assay
ChEMBL 444 6 0 10 2.7 CCOC(=O)C1CCN(c2ncnc(Oc3cc(C(F)(F)F)nn3C)c2[N+](=O)[O-])CC1 10.1021/jm8006867
46208490 89064 0 None - 0 Human 7.7 pKi = 7.7 Functional
Agonist activity at GPR119Agonist activity at GPR119
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3COC[C@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm300343m
CHEMBL2171708 89064 0 None - 0 Human 7.7 pKi = 7.7 Functional
Agonist activity at GPR119Agonist activity at GPR119
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3COC[C@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm300343m
11705608 7224 65 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.
Guide to Pharmacology 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 21444206
12151 7224 65 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.
Guide to Pharmacology 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 21444206
CHEMBL1775179 7224 65 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.
Guide to Pharmacology 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 21444206
11705608 7224 65 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.
Guide to Pharmacology 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 21444206
12151 7224 65 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.
Guide to Pharmacology 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 21444206
CHEMBL1775179 7224 65 None -6 2 Rat 7.5 pEC50 = 7.5 Functional
Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.Determined in a melanophore assay (<i>Xenopus</i> oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion.
Guide to Pharmacology 477 5 0 9 2.7 CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2c1cnn2c1c(cc(cc1)S(=O)(=O)C)F 21444206
10137 10883 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Measuring agonist-induced stimulation of cAMP accumulation.Measuring agonist-induced stimulation of cAMP accumulation.
Guide to Pharmacology 545 6 0 12 2.9 N#Cc1cc(cnc1N1CCN(CC1)c1noc(n1)C(C)C)c1ccc(c(c1)F)n1cnn(c1=O)[C@@H]1COCC1 29495245
86281591 10883 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Measuring agonist-induced stimulation of cAMP accumulation.Measuring agonist-induced stimulation of cAMP accumulation.
Guide to Pharmacology 545 6 0 12 2.9 N#Cc1cc(cnc1N1CCN(CC1)c1noc(n1)C(C)C)c1ccc(c(c1)F)n1cnn(c1=O)[C@@H]1COCC1 29495245
10082 8271 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Measuring concentration-dependent increased intracellular cAMPMeasuring concentration-dependent increased intracellular cAMP
Guide to Pharmacology 467 10 2 7 4.1 CC[C@H](c1onc(n1)c1ccc(c(c1)F)C(=O)N[C@@H](CO)C)Oc1ccc(cc1)C(=O)C1CC1 30217957
56959560 8271 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Measuring concentration-dependent increased intracellular cAMPMeasuring concentration-dependent increased intracellular cAMP
Guide to Pharmacology 467 10 2 7 4.1 CC[C@H](c1onc(n1)c1ccc(c(c1)F)C(=O)N[C@@H](CO)C)Oc1ccc(cc1)C(=O)C1CC1 30217957
2488 9699 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 18 2 3 7.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCc1ccc(c(c1)OC)O 19901198
5311093 9699 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 18 2 3 7.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCc1ccc(c(c1)OC)O 19901198
CHEMBL76903 9699 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 18 2 3 7.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCc1ccc(c(c1)OC)O 19901198
2875918 9996 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 5 0 4 4.6 CCCCC1CCC(CC1)c1onc(n1)c1ccncc1 16517404
3318 9996 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 5 0 4 4.6 CCCCC1CCC(CC1)c1onc(n1)c1ccncc1 16517404
CHEMBL4303425 9996 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 5 0 4 4.6 CCCCC1CCC(CC1)c1onc(n1)c1ccncc1 16517404
5652 9211 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 8 2 8 -1.6 [O-]P(=O)(OCCN)OC[C@@H](COC(=O)C)O 15607732
73755142 9211 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 8 2 8 -1.6 [O-]P(=O)(OCCN)OC[C@@H](COC(=O)C)O 15607732
4028 9212 0 None -15 2 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 7 7 11 -3.8 O[C@@H](COC(=O)C)COP(=O)(O[C@@H]1[C@H](O)[C@H](O)[C@H]([C@@H]([C@H]1O)O)O)O 15607732
73755067 9212 0 None -15 2 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 7 7 11 -3.8 O[C@@H](COC(=O)C)COP(=O)(O[C@@H]1[C@H](O)[C@H](O)[C@H]([C@@H]([C@H]1O)O)O)O 15607732
10166 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 24751443
25025505 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 24751443
CHEMBL3260505 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 24751443
DB12345 9245 65 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 7 0 10 3.4 CCc1cnc(nc1)N1CCC(CC1)c1scc(n1)COc1ccc(cc1)n1cnnn1 24751443
11462546 9997 43 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 16517404
3319 9997 43 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 16517404
CHEMBL1081913 9997 43 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 7 3.0 O=C(N1CCC(CC1)OCc1onc(n1)c1ccncc1)OC(C)(C)C 16517404
54580880 7800 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 4 3.9 O=C(N1CCC(CC1)C1CCN(CC1)c1cccnc1)OC(C)(C)C 21273063
5745 7800 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 4 3.9 O=C(N1CCC(CC1)C1CCN(CC1)c1cccnc1)OC(C)(C)C 21273063
CHEMBL1770918 7800 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 4 3.9 O=C(N1CCC(CC1)C1CCN(CC1)c1cccnc1)OC(C)(C)C 21273063
497299 6829 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 25 1 7 5.4 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
5651 6829 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 25 1 7 5.4 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
CHEMBL3093101 6829 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 25 1 7 5.4 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
5282106 9629 32 None -1 2 Human 5.5 pEC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 18 3 3 6.8 CCCCCCCC/C=C\CCCCCCCC(=O)NCCc1ccc(c(c1)O)O 19901198
5552 9629 32 None -1 2 Human 5.5 pEC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 18 3 3 6.8 CCCCCCCC/C=C\CCCCCCCC(=O)NCCc1ccc(c(c1)O)O 19901198
CHEMBL250711 9629 32 None -1 2 Human 5.5 pEC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 18 3 3 6.8 CCCCCCCC/C=C\CCCCCCCC(=O)NCCc1ccc(c(c1)O)O 19901198
10200069 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 20937249
10200069 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 21114601
10200069 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 22365911
5722 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 20937249
5722 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 21114601
5722 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 22365911
CHEMBL1956608 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 20937249
CHEMBL1956608 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 21114601
CHEMBL1956608 7268 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 4 3.5 Brc1ccc(cc1)c1nc(NCCc2ccc[n+](c2)[O-])cc(n1)C 22365911
5283468 6826 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(CO)O 21778222
5756 6826 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(CO)O 21778222
CHEMBL428593 6826 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(CO)O 21778222
DB13171 6826 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(CO)O 21778222
5112 6872 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC(CO)CO 21778222
5319879 6872 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC(CO)CO 21778222
CHEMBL3182200 6872 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 18 2 4 4.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC(CO)CO 21778222
4027 7267 59 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 2 4 2.6 OCCNc1cc(C)nc(n1)c1ccc(cc1)Br 20804735
5332859 7267 59 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 2 4 2.6 OCCNc1cc(C)nc(n1)c1ccc(cc1)Br 20804735
CHEMBL1956589 7267 59 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 4 2 4 2.6 OCCNc1cc(C)nc(n1)c1ccc(cc1)Br 20804735
10097314 6827 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 495 23 1 7 4.6 CCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
5650 6827 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 495 23 1 7 4.6 CCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
16081932 9692 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 521 24 1 7 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
3623 9692 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 521 24 1 7 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
CHEMBL3093102 9692 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 521 24 1 7 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COP(=O)(OCC[N+](C)(C)C)[O-])O 15607732
2661 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 16517404
2661 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 19901198
2661 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 23396314
5283454 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 16517404
5283454 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 19901198
5283454 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 23396314
CHEMBL280065 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 16517404
CHEMBL280065 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 19901198
CHEMBL280065 9630 65 None -4 4 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 23396314
11567371 7271 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 6 1 6 2.6 OC(=O)CCCC1CCN(CC1)c1nc(nc2c1CS(=O)(=O)C2)C1CCC1 20816753
5723 7271 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 6 1 6 2.6 OC(=O)CCCC1CCN(CC1)c1nc(nc2c1CS(=O)(=O)C2)C1CCC1 20816753
5743 7801 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 3 0 7 3.2 N#Cc1cc(cnc1N1CCN(CC1)C(=O)OC(C)C)c1ccc2c(c1)nccn2 21939274
73755151 7801 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 3 0 7 3.2 N#Cc1cc(cnc1N1CCN(CC1)C(=O)OC(C)C)c1ccc2c(c1)nccn2 21939274
CHEMBL4583018 7801 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 3 0 7 3.2 N#Cc1cc(cnc1N1CCN(CC1)C(=O)OC(C)C)c1ccc2c(c1)nccn2 21939274
10410511 10407 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 431 19 3 3 6.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](Cc1ccc(cc1)O)CO 19901198
5721 10407 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 431 19 3 3 6.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](Cc1ccc(cc1)O)CO 19901198
CHEMBL1534468 10407 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 431 19 3 3 6.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](Cc1ccc(cc1)O)CO 19901198
5720 10110 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 431 19 3 3 6.4 CCCCCCCC/C=C/CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)O)CO 19901198
73755147 10110 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 431 19 3 3 6.4 CCCCCCCC/C=C/CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)O)CO 19901198
51346816 7876 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 6 1 3 3.5 O=C(Cc1c(F)ccc(c1F)F)NC[C@H](C1CCN(CC1)C(=O)OC1(C)CC1)F 21310611
5724 7876 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 6 1 3 3.5 O=C(Cc1c(F)ccc(c1F)F)NC[C@H](C1CCN(CC1)C(=O)OC1(C)CC1)F 21310611
CHEMBL1683943 7876 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 6 1 3 3.5 O=C(Cc1c(F)ccc(c1F)F)NC[C@H](C1CCN(CC1)C(=O)OC1(C)CC1)F 21310611
11691484 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 22264481
5727 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 22264481
CHEMBL1951032 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 22264481
DB12084 8921 51 None 8 2 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 7 1 10 2.7 COc1c(ncnc1Nc1ccc(nc1C)S(=O)(=O)C)OC1CCN(CC1)C(=O)OC(C)C 22264481
5747 7862 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 3 0 6 3.0 C#Cc1nc(C)cc(n1)N1CCC(CC1)C1CCN(CC1)c1ncc(nc1)C 21273063
73755153 7862 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 3 0 6 3.0 C#Cc1nc(C)cc(n1)N1CCC(CC1)C1CCN(CC1)c1ncc(nc1)C 21273063
54585570 7810 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 426 4 0 7 4.6 O=C(N1[C@H]2CC[C@H]1CC(C2)Oc1ncnc(c1C)Oc1cccnc1C)OC(C)(C)C 21536438
5750 7810 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 426 4 0 7 4.6 O=C(N1[C@H]2CC[C@H]1CC(C2)Oc1ncnc(c1C)Oc1cccnc1C)OC(C)(C)C 21536438
5735 7883 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 0 10 2.5 N#Cc1cnccc1COc1cnc(nc1)N1CCN(C[C@@H]1C)c1noc(n1)C(C)C 22545772
60168163 7883 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 0 10 2.5 N#Cc1cnccc1COc1cnc(nc1)N1CCN(C[C@@H]1C)c1noc(n1)C(C)C 22545772
24939268 7240 67 None - 1 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 17289847
5653 7240 67 None - 1 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 17289847
CHEMBL461384 7240 67 None - 1 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 17289847
53235534 7905 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 21273063
5748 7905 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 21273063
CHEMBL1771100 7905 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 7 0 7 3.3 Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)S(=O)(=O)C 21273063
54587590 7860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 473 6 1 7 3.9 N#Cc1ccc(c(c1)Cl)Nc1ncnc(c1C)OC1C[C@@H]2CC[C@@H](C1)N2S(=O)(=O)C1CC1 21536438
5755 7860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 473 6 1 7 3.9 N#Cc1ccc(c(c1)Cl)Nc1ncnc(c1C)OC1C[C@@H]2CC[C@@H](C1)N2S(=O)(=O)C1CC1 21536438
CHEMBL1778248 7860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 473 6 1 7 3.9 N#Cc1ccc(c(c1)Cl)Nc1ncnc(c1C)OC1C[C@@H]2CC[C@@H](C1)N2S(=O)(=O)C1CC1 21536438
5744 7848 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 4 0 7 4.7 N#Cc1cc(cnc1N1CCC(CC1)c1onc(n1)C(C)C)c1ccc(c(c1)C)C#N 21939274
73755152 7848 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 4 0 7 4.7 N#Cc1cc(cnc1N1CCC(CC1)c1onc(n1)C(C)C)c1ccc(c(c1)C)C#N 21939274
11282871 7870 0 None 8 2 Human 9.0 pEC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 21444206
5737 7870 0 None 8 2 Human 9.0 pEC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 21444206
CHEMBL1775169 7870 0 None 8 2 Human 9.0 pEC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 473 4 0 9 3.0 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 21444206
53630394 7873 0 None 21 2 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
5738 7873 0 None 21 2 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
CHEMBL1775178 7873 0 None 21 2 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 4 0 9 3.1 O=C(N1CCC(CC1)Oc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
11397354 7839 2 None 23 2 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 21444206
5741 7839 2 None 23 2 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 21444206
CHEMBL1773293 7839 2 None 23 2 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 474 4 0 9 3.5 O=C(N1CCC(CC1)Oc1ncnc2c1onc2c1ccc(cc1)S(=O)(=O)C)OC(C)(C)C 21444206
54582152 7827 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 4 1 9 2.4 O=C(N1CCC(CC1)Oc1ncnc2c1[nH]c(=O)n2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
5740 7827 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 4 1 9 2.4 O=C(N1CCC(CC1)Oc1ncnc2c1[nH]c(=O)n2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
CHEMBL1773292 7827 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 4 1 9 2.4 O=C(N1CCC(CC1)Oc1ncnc2c1[nH]c(=O)n2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
53630410 7928 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
5739 7928 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206
CHEMBL1773283 7928 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 4 0 9 3.9 O=C(N1CCC(CC1)Sc1ncnc2c1cnn2c1ccc(cc1F)S(=O)(=O)C)OC(C)(C)C 21444206




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

155568284 182889 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 440 3 0 7 3.8 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(C(F)(F)F)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4591642 182889 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 440 3 0 7 3.8 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(C(F)(F)F)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
57468373 121448 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 453 6 0 7 3.2 CCc1ccc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338170 121448 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 453 6 0 7 3.2 CCc1ccc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
25204244 121442 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 448 5 0 7 3.0 CC(C)OC(=O)N1CCCC(Oc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
CHEMBL3338164 121442 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 448 5 0 7 3.0 CC(C)OC(=O)N1CCCC(Oc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
57468459 121454 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 415 6 0 7 3.5 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(C#N)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338176 121454 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 415 6 0 7 3.5 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(C#N)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
155536150 178917 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 474 3 0 7 4.5 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(C(F)(F)F)cc3Cl)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4473081 178917 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 474 3 0 7 4.5 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(C(F)(F)F)cc3Cl)nn2)CC1 10.1016/j.bmcl.2019.126707
57468382 121450 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 456 6 0 9 2.1 COc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338172 121450 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 456 6 0 9 2.1 COc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
57550101 121462 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 493 7 0 9 2.9 CCCc1cnc(N2CCC(Oc3cc(=O)n(-c4ccc(S(C)(=O)=O)cc4)cc3C#N)CC2)nc1 10.1021/jm501175v
CHEMBL3338187 121462 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 493 7 0 9 2.9 CCCc1cnc(N2CCC(Oc3cc(=O)n(-c4ccc(S(C)(=O)=O)cc4)cc3C#N)CC2)nc1 10.1021/jm501175v
53477049 121465 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 546 5 0 8 3.9 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(C(F)(F)F)cn4)CC3)cc2=O)c(F)c1 10.1021/jm501175v
CHEMBL3338190 121465 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 546 5 0 8 3.9 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(C(F)(F)F)cn4)CC3)cc2=O)c(F)c1 10.1021/jm501175v
155528272 178094 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 474 3 0 7 4.5 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(Cl)c(C(F)(F)F)c3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4461083 178094 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 474 3 0 7 4.5 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(Cl)c(C(F)(F)F)c3)nn2)CC1 10.1016/j.bmcl.2019.126707
155525761 177801 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 459 2 0 6 3.6 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(Cl)c(C(F)(F)F)c3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4456666 177801 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 459 2 0 6 3.6 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(Cl)c(C(F)(F)F)c3)nn2)CC1 10.1016/j.bmcl.2019.126707
155528891 178150 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 453 3 0 8 1.5 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4461803 178150 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 453 3 0 8 1.5 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
162663470 188732 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4779950 188732 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at rat GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
53477048 121464 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 528 5 0 8 3.8 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(C(F)(F)F)cn4)CC3)cc2=O)cc1 10.1021/jm501175v
CHEMBL3338189 121464 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 528 5 0 8 3.8 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(C(F)(F)F)cn4)CC3)cc2=O)cc1 10.1021/jm501175v
53390936 121468 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 512 5 0 8 3.5 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)cc1F 10.1021/jm501175v
CHEMBL3338193 121468 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 512 5 0 8 3.5 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)cc1F 10.1021/jm501175v
155530371 178342 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 425 2 0 6 3.0 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(C(F)(F)F)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4464713 178342 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 425 2 0 6 3.0 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(C(F)(F)F)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
155523981 177685 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 468 4 0 9 2.4 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4454792 177685 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 468 4 0 9 2.4 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
25204713 121446 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 468 5 0 7 3.3 CS(=O)(=O)c1ccc(-n2ccc(OC3CCN(C(=O)Oc4ccccc4)CC3)cc2=O)cc1 10.1021/jm501175v
CHEMBL3338168 121446 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 468 5 0 7 3.3 CS(=O)(=O)c1ccc(-n2ccc(OC3CCN(C(=O)Oc4ccccc4)CC3)cc2=O)cc1 10.1021/jm501175v
25138357 121443 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 434 5 0 7 2.6 CC(C)OC(=O)N1CCC(Oc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
CHEMBL3338165 121443 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 434 5 0 7 2.6 CC(C)OC(=O)N1CCC(Oc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
53477157 121469 14 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 512 5 0 8 3.5 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)c(F)c1 10.1021/jm501175v
CHEMBL3338194 121469 14 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 512 5 0 8 3.5 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)c(F)c1 10.1021/jm501175v
162656652 187617 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 7 1 8 3.4 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc([S+]([O-])CCO)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
CHEMBL4757058 187617 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 7 1 8 3.4 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc([S+]([O-])CCO)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
68230201 129065 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 402 4 0 7 3.5 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(C#N)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598092 129065 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 402 4 0 7 3.5 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(C#N)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
67607375 90447 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 448 6 0 10 2.6 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)CC1 10.1021/ml300296q
CHEMBL2204983 90447 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 448 6 0 10 2.6 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)CC1 10.1021/ml300296q
162675131 190183 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 505 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCOCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4798241 190183 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 505 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCOCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
25204038 121452 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 468 7 0 8 3.0 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338174 121452 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 468 7 0 8 3.0 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
53477155 121466 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 546 5 0 8 3.9 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(C(F)(F)F)cn4)CC3)cc2=O)cc1F 10.1021/jm501175v
CHEMBL3338191 121466 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 546 5 0 8 3.9 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(C(F)(F)F)cn4)CC3)cc2=O)cc1F 10.1021/jm501175v
162663470 188732 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4779950 188732 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
25260830 111854 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
CHEMBL3113840 111854 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 460 5 0 8 3.0 CC(C)OC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
162658401 187860 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCC(O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4759952 187860 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCC(O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
162675059 190039 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 503 6 0 9 4.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4796498 190039 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 503 6 0 9 4.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
25204242 121440 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 448 6 0 7 2.9 CC(C)OC(=O)N1CCC(COc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
CHEMBL3338159 121440 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 448 6 0 7 2.9 CC(C)OC(=O)N1CCC(COc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
57550042 121459 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 486 7 0 8 3.2 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4F)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338181 121459 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 486 7 0 8 3.2 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4F)c(=O)c3)CC2)nc1 10.1021/jm501175v
53477156 121467 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 494 5 0 8 3.4 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)cc1 10.1021/jm501175v
CHEMBL3338192 121467 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 494 5 0 8 3.4 CS(=O)(=O)c1ccc(-n2cc(Cl)c(OC3CCN(c4ncc(Cl)cn4)CC3)cc2=O)cc1 10.1021/jm501175v
25204174 121445 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 448 4 0 7 3.0 CC(C)(C)OC(=O)N1CCC(Oc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
CHEMBL3338167 121445 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 448 4 0 7 3.0 CC(C)(C)OC(=O)N1CCC(Oc2ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c2)CC1 10.1021/jm501175v
162663470 188732 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at GPR119 in glucose-induced mouse L cells assessed as induction of GLP-1 secretion after 2 hrs by ELISAAgonist activity at GPR119 in glucose-induced mouse L cells assessed as induction of GLP-1 secretion after 2 hrs by ELISA
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4779950 188732 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at GPR119 in glucose-induced mouse L cells assessed as induction of GLP-1 secretion after 2 hrs by ELISAAgonist activity at GPR119 in glucose-induced mouse L cells assessed as induction of GLP-1 secretion after 2 hrs by ELISA
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
25052772 166072 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 491 4 1 10 3.1 CC(C)(C)OC(=O)N1CCC(n2nnc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc32)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL4099566 166072 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 491 4 1 10 3.1 CC(C)(C)OC(=O)N1CCC(n2nnc3c(Nc4ccc(S(C)(=O)=O)cc4F)ncnc32)CC1 10.1016/j.bmcl.2017.06.034
CHEMBL5266838 200274 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human GPR119 expressed in CHO-K1 cells assessed as increase in intracellular cAMP level incubated for 5 mins by fluorescence analysisAgonist activity at human GPR119 expressed in CHO-K1 cells assessed as increase in intracellular cAMP level incubated for 5 mins by fluorescence analysis
ChEMBL 322 3 2 6 1.0 O=c1[nH]ncn1-c1ccc(-c2ccc(N3CCNCC3)nc2)cc1 10.1016/j.ejmech.2018.04.061
16733804 147297 1 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assayAgonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assay
ChEMBL 415 6 0 5 4.0 CC(C)(C)OC(=O)N1CCC(CCCOc2ccc(S(C)(=O)=O)c(F)c2)CC1 10.1021/acs.jmedchem.5b01198
CHEMBL3810173 147297 1 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assayAgonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assay
ChEMBL 415 6 0 5 4.0 CC(C)(C)OC(=O)N1CCC(CCCOc2ccc(S(C)(=O)=O)c(F)c2)CC1 10.1021/acs.jmedchem.5b01198
53492528 129056 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598083 129056 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 471 5 0 6 4.3 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(S(C)(=O)=O)cc3F)CC2)CC1 10.1016/j.bmcl.2015.04.102
25204037 121451 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 466 6 0 8 3.0 CS(=O)(=O)c1ccc(-n2ccc(OC3CCN(c4ncc(C5CC5)cn4)CC3)cc2=O)cc1 10.1021/jm501175v
CHEMBL3338173 121451 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 466 6 0 8 3.0 CS(=O)(=O)c1ccc(-n2ccc(OC3CCN(c4ncc(C5CC5)cn4)CC3)cc2=O)cc1 10.1021/jm501175v
162659593 188159 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 540 6 1 10 2.8 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCNS6(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4763323 188159 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 540 6 1 10 2.8 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCNS6(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL5275303 200627 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119 expressed in HEK293S cells assessed as increase in intracellular cAMP level incubated for 45 mins by HTRF analysisAgonist activity at human GPR119 expressed in HEK293S cells assessed as increase in intracellular cAMP level incubated for 45 mins by HTRF analysis
ChEMBL 568 10 0 9 6.2 CSc1ccc(COc2ccc(-c3ncc(C)c(N4CCN(c5ncc(OCC=C(C)C)cn5)CC4)n3)cc2)cc1 10.1016/j.ejmech.2018.04.061
162663470 188732 0 None - 0 Golden hamster 7.6 pEC50 = 7.6 Binding
Agonist activity at GPR119 in glucose-induced golden hamster HIT-T15 cells assessed as increase in insulin secretion after 2 hrs by A1phaLISAAgonist activity at GPR119 in glucose-induced golden hamster HIT-T15 cells assessed as increase in insulin secretion after 2 hrs by A1phaLISA
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4779950 188732 0 None - 0 Golden hamster 7.6 pEC50 = 7.6 Binding
Agonist activity at GPR119 in glucose-induced golden hamster HIT-T15 cells assessed as increase in insulin secretion after 2 hrs by A1phaLISAAgonist activity at GPR119 in glucose-induced golden hamster HIT-T15 cells assessed as increase in insulin secretion after 2 hrs by A1phaLISA
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
162644623 186170 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4739871 186170 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC[C@@H](O)C6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
156014644 184005 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 545 5 2 8 5.0 CC(C)(C)OC(=O)N1C2CCC1CC(Nc1nc(Nc3ccc(S(C)(=O)=O)cc3F)nc3c1CCCC3)C2 10.1016/j.bmc.2019.115263
CHEMBL4635583 184005 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 545 5 2 8 5.0 CC(C)(C)OC(=O)N1C2CCC1CC(Nc1nc(Nc3ccc(S(C)(=O)=O)cc3F)nc3c1CCCC3)C2 10.1016/j.bmc.2019.115263
122184150 129089 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
CHEMBL3598115 129089 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
68230358 129078 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 461 7 0 7 2.6 CCC(F)(F)C(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598104 129078 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 461 7 0 7 2.6 CCC(F)(F)C(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
2661 9630 65 None - 3 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assayAgonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1021/acs.jmedchem.5b01198
5283454 9630 65 None - 3 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assayAgonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1021/acs.jmedchem.5b01198
CHEMBL280065 9630 65 None - 3 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assayAgonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assay
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1021/acs.jmedchem.5b01198
155513850 176594 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 435 3 0 8 1.4 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4439483 176594 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 435 3 0 8 1.4 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
58074106 188591 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 476 5 0 8 3.7 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
CHEMBL4778132 188591 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 476 5 0 8 3.7 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc(S(C)(=O)=O)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
155565475 182335 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 415 3 0 8 2.8 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(C#N)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4578862 182335 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 415 3 0 8 2.8 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(C#N)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
155537620 179082 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 450 4 0 9 2.2 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4475130 179082 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 450 4 0 9 2.2 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3ccc(S(C)(=O)=O)cc3)nn2)CC1 10.1016/j.bmcl.2019.126707
76314115 111681 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 6 0 7 3.6 CCc1cnc(N2CCC(C(C)COC(=O)N3CCc4cc(S(C)(=O)=O)cc(F)c43)CC2)nc1 10.1016/j.bmc.2021.116034
CHEMBL3112602 111681 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 6 0 7 3.6 CCc1cnc(N2CCC(C(C)COC(=O)N3CCc4cc(S(C)(=O)=O)cc(F)c43)CC2)nc1 10.1016/j.bmc.2021.116034
CHEMBL5284750 201040 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human GPR119 incubated for 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 incubated for 2 hrs by luciferase reporter gene assay
ChEMBL 472 6 0 7 3.5 CCc1cnc(N2CCC(C(C)COC(=O)N3CCc4cc(S(C)(=O)=O)ccc43)CC2)nc1 10.1016/j.ejmech.2021.113665
67606673 90450 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 423 5 0 7 3.7 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)CC1 10.1021/ml300296q
CHEMBL2204986 90450 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 423 5 0 7 3.7 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)CC1 10.1021/ml300296q
57468398 121461 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 482 7 0 8 3.3 CCCc1cnc(N2CCC(Oc3cc(=O)n(-c4ccc(S(C)(=O)=O)cc4)cc3C)CC2)nc1 10.1021/jm501175v
CHEMBL3338185 121461 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 482 7 0 8 3.3 CCCc1cnc(N2CCC(Oc3cc(=O)n(-c4ccc(S(C)(=O)=O)cc4)cc3C)CC2)nc1 10.1021/jm501175v
57468435 121456 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 473 7 0 7 3.8 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(N5CCCC5=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338178 121456 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 473 7 0 7 3.8 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(N5CCCC5=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
2661 9630 65 None - 3 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant GPR119 receptor (unknown origin)Agonist activity at recombinant GPR119 receptor (unknown origin)
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1021/jm300484d
5283454 9630 65 None - 3 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant GPR119 receptor (unknown origin)Agonist activity at recombinant GPR119 receptor (unknown origin)
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1021/jm300484d
CHEMBL280065 9630 65 None - 3 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant GPR119 receptor (unknown origin)Agonist activity at recombinant GPR119 receptor (unknown origin)
ChEMBL 325 17 2 2 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)NCCO 10.1021/jm300484d
58074114 189407 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 489 6 0 9 3.9 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4788517 189407 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 489 6 0 9 3.9 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
53491642 129058 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 400 4 0 5 4.7 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(C#N)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598085 129058 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 400 4 0 5 4.7 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3ccc(C#N)cc3)CC2)CC1 10.1016/j.bmcl.2015.04.102
57550050 121444 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 460 5 0 7 3.2 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c1)C2 10.1021/jm501175v
CHEMBL3338166 121444 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 460 5 0 7 3.2 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c1)C2 10.1021/jm501175v
162647887 190418 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 504 6 1 10 2.7 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCNCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4746627 190418 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 504 6 1 10 2.7 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCNCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4802539 190418 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 504 6 1 10 2.7 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCNCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
57550087 121455 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 489 7 1 7 4.6 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(NC(=O)C(C)(C)C)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338177 121455 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 489 7 1 7 4.6 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(NC(=O)C(C)(C)C)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
68230212 129072 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598099 129072 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 495 6 0 8 3.1 C[C@@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
155511104 176311 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 400 2 0 7 2.0 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(C#N)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4435207 176311 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 400 2 0 7 2.0 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(C#N)cc3F)nn2)CC1 10.1016/j.bmcl.2019.126707
24939268 7240 67 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2019.126707
5653 7240 67 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2019.126707
CHEMBL461384 7240 67 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 505 7 1 11 3.6 O=N(=O)c1c(ncnc1N1CCC(CC1)c1onc(n1)C(C)C)Nc1ccc(cc1F)S(=O)(=O)C 10.1016/j.bmcl.2019.126707
24862850 147257 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assayAgonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assay
ChEMBL 469 5 0 8 3.8 C[C@H](OC1CCN(C(=O)OC(C)(C)C)CC1)c1nc(-c2ccc(S(C)(=O)=O)c(F)c2)no1 10.1021/acs.jmedchem.5b01198
CHEMBL3809616 147257 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assayAgonist activity at human GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after by fluorescent reporter gene assay
ChEMBL 469 5 0 8 3.8 C[C@H](OC1CCN(C(=O)OC(C)(C)C)CC1)c1nc(-c2ccc(S(C)(=O)=O)c(F)c2)no1 10.1021/acs.jmedchem.5b01198
57550070 121453 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 452 7 0 7 3.4 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc([S+](C)[O-])cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338175 121453 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 452 7 0 7 3.4 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc([S+](C)[O-])cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
162653364 187224 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 514 8 1 11 2.5 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(=O)(=O)CCO)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4752544 187224 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 514 8 1 11 2.5 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(=O)(=O)CCO)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
53492331 129075 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 549 6 0 8 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C(F)(F)F)C(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
CHEMBL3598101 129075 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 549 6 0 8 3.7 CS(=O)(=O)c1cnc(O[C@H]2CC[C@H](OC3CCN(C(=O)OC(C(F)(F)F)C(F)(F)F)CC3)CC2)cn1 10.1016/j.bmcl.2015.04.102
162663885 188783 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 502 6 0 9 5.0 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(C6CCCCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4780567 188783 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 502 6 0 9 5.0 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(C6CCCCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
162670073 189527 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 498 8 1 10 2.8 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc([S+]([O-])CCO)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4790055 189527 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 498 8 1 10 2.8 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc([S+]([O-])CCO)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
57468427 121463 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 502 7 0 8 3.7 CCCc1cnc(N2CCC(Oc3cc(=O)n(-c4ccc(S(C)(=O)=O)cc4)cc3Cl)CC2)nc1 10.1021/jm501175v
CHEMBL3338188 121463 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 502 7 0 8 3.7 CCCc1cnc(N2CCC(Oc3cc(=O)n(-c4ccc(S(C)(=O)=O)cc4)cc3Cl)CC2)nc1 10.1021/jm501175v
67950429 90448 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 456 7 0 11 2.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)nc1 10.1021/ml300296q
CHEMBL2204984 90448 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 456 7 0 11 2.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)nc1 10.1021/ml300296q
67633261 90449 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 431 6 0 8 3.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)nc1 10.1021/ml300296q
CHEMBL2204985 90449 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 431 6 0 8 3.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)nc1 10.1021/ml300296q
53492264 129074 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 495 6 0 8 3.1 C[C@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
CHEMBL3598100 129074 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 495 6 0 8 3.1 C[C@H](OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1)C(F)(F)F 10.1016/j.bmcl.2015.04.102
122184148 129087 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 479 8 0 10 2.8 CC(C)c1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
CHEMBL3598113 129087 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 479 8 0 10 2.8 CC(C)c1nc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)no1 10.1016/j.bmcl.2015.04.102
25204645 121447 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 454 6 0 8 2.6 CCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338169 121447 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 454 6 0 8 2.6 CCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
162656652 187617 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 7 1 8 3.4 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc([S+]([O-])CCO)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
CHEMBL4757058 187617 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 7 1 8 3.4 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc([S+]([O-])CCO)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
122184149 129088 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
CHEMBL3598114 129088 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 497 9 0 10 2.5 CC(F)Cc1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
58114293 90446 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
CHEMBL2204982 90446 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysisAgonist activity at GPR119 in human U20S cells assessed as binding to beta-arrestin by chemiluminescence analysis
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
25138367 121457 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 457 7 0 9 3.2 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(-n5cncn5)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338179 121457 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 457 7 0 9 3.2 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(-n5cncn5)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
122184147 129086 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 479 8 0 10 2.8 CC(C)c1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
CHEMBL3598112 129086 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 479 8 0 10 2.8 CC(C)c1noc(CN2CCC(O[C@H]3CC[C@H](Oc4cnc(S(C)(=O)=O)cn4)CC3)CC2)n1 10.1016/j.bmcl.2015.04.102
155525822 177842 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 414 2 0 8 2.6 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3nc4ccccc4s3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4457078 177842 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 414 2 0 8 2.6 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3nc4ccccc4s3)nn2)CC1 10.1016/j.bmcl.2019.126707
46897575 111794 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 484 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL3113623 111794 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 484 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
46897575 111794 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR119 incubated for 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 incubated for 2 hrs by luciferase reporter gene assay
ChEMBL 484 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.ejmech.2021.113665
CHEMBL3113623 111794 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR119 incubated for 2 hrs by luciferase reporter gene assayAgonist activity at human GPR119 incubated for 2 hrs by luciferase reporter gene assay
ChEMBL 484 6 0 10 3.1 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(S(C)(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.ejmech.2021.113665
25204648 121449 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 440 5 0 8 2.4 Cc1ccnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)n1 10.1021/jm501175v
CHEMBL3338171 121449 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 440 5 0 8 2.4 Cc1ccnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)cc4)c(=O)c3)CC2)n1 10.1021/jm501175v
162656085 187483 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 477 6 0 9 3.7 CC(=O)N(C)c1ccc2c(c1)CCN2c1cc(OC2CCN(c3nc(C(C)C)no3)CC2)ncn1 10.1016/j.bmc.2021.116034
CHEMBL4755582 187483 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 477 6 0 9 3.7 CC(=O)N(C)c1ccc2c(c1)CCN2c1cc(OC2CCN(c3nc(C(C)C)no3)CC2)ncn1 10.1016/j.bmc.2021.116034
155542312 179919 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 429 3 0 9 3.4 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3nc4ccccc4s3)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4521163 179919 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 429 3 0 9 3.4 CC(C)(C)OC(=O)N1CCC(OC(=O)c2cn(-c3nc4ccccc4s3)nn2)CC1 10.1016/j.bmcl.2019.126707
155517636 176981 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 459 2 0 6 3.6 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(C(F)(F)F)cc3Cl)nn2)CC1 10.1016/j.bmcl.2019.126707
CHEMBL4445174 176981 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assayAgonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
ChEMBL 459 2 0 6 3.6 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn(-c3ccc(C(F)(F)F)cc3Cl)nn2)CC1 10.1016/j.bmcl.2019.126707
137647821 164337 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 511 7 1 11 3.1 CCCc1cnc(N2CCC(n3nnc4c(Nc5ccc(S(C)(=O)=O)cc5F)ncnc43)CC2)nc1 10.1016/j.bmcl.2017.06.034
CHEMBL4080356 164337 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 511 7 1 11 3.1 CCCc1cnc(N2CCC(n3nnc4c(Nc5ccc(S(C)(=O)=O)cc5F)ncnc43)CC2)nc1 10.1016/j.bmcl.2017.06.034
57550050 121444 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 460 5 0 7 3.2 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c1)C2 10.1021/jm501175v
CHEMBL3338166 121444 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 460 5 0 7 3.2 CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(Oc1ccn(-c3ccc(S(C)(=O)=O)cc3)c(=O)c1)C2 10.1021/jm501175v
162662520 188754 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC(O)CC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4780236 188754 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCC(O)CC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
57468409 121460 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 486 7 0 8 3.2 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)c(F)c4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338182 121460 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 486 7 0 8 3.2 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(S(C)(=O)=O)c(F)c4)c(=O)c3)CC2)nc1 10.1021/jm501175v
162656652 187617 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 7 1 8 3.4 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc([S+]([O-])CCO)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
CHEMBL4757058 187617 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 490 7 1 8 3.4 CC(C)SC(=O)N1CCC(Oc2cc(N3CCc4cc([S+]([O-])CCO)ccc43)ncn2)CC1 10.1016/j.bmc.2021.116034
162657827 187907 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 525 6 0 10 3.3 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCS6(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4760572 187907 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 525 6 0 10 3.3 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CCCS6(=O)=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
162654626 187421 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CC(O)CCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
CHEMBL4754973 187421 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assayAgonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element incubated for 2 hrs by steady-glo luciferase assay
ChEMBL 519 6 1 10 3.2 CC(C)c1noc(N2CCC(Oc3cc(N4CCc5cc(N6CC(O)CCC6=O)ccc54)ncn3)CC2)n1 10.1016/j.bmc.2021.116034
54596144 129067 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 441 6 0 8 2.6 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598094 129067 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 441 6 0 8 2.6 CC(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
53492594 129063 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
CHEMBL3598090 129063 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119 by serum shift assayAgonist activity at human GPR119 by serum shift assay
ChEMBL 455 5 0 8 3.0 CC(C)(C)OC(=O)N1CCC(O[C@H]2CC[C@H](Oc3cnc(S(C)(=O)=O)cn3)CC2)CC1 10.1016/j.bmcl.2015.04.102
42646474 121458 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 456 7 0 8 3.8 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(-n5ccnc5)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
CHEMBL3338180 121458 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR119Agonist activity at human GPR119
ChEMBL 456 7 0 8 3.8 CCCc1cnc(N2CCC(Oc3ccn(-c4ccc(-n5ccnc5)cc4)c(=O)c3)CC2)nc1 10.1021/jm501175v
51030054 84194 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086684 84194 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
73350444 96972 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 4 0 8 2.9 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1016/j.bmcl.2013.04.006
CHEMBL2382410 96972 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 4 0 8 2.9 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1016/j.bmcl.2013.04.006
51030053 84191 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086680 84191 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
51030054 84194 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086684 84194 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 410 4 0 8 2.8 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
73353420 96977 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382415 96977 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
51030710 96978 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382416 96978 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
73351961 96979 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382417 96979 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
51029876 84172 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086660 84172 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
51029876 84172 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086660 84172 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 462 5 0 8 2.9 C[C@@H]1CN(C(=O)OC(C)(C)C)CCN1c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
51030985 96976 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382414 96976 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
51030984 84197 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086687 84197 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL5271736 200474 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of GPR119 (unknown origin) at 10 uMInhibition of GPR119 (unknown origin) at 10 uM
ChEMBL 320 3 2 6 3.3 Nc1nc(Nc2ccc(F)cc2)n2nc(-c3ccccc3)cc2n1 10.1016/j.ejmech.2021.113537
72188621 96973 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382411 96973 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
51030710 96978 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382416 96978 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 406 6 0 10 2.2 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)CC2)no1 10.1016/j.bmcl.2013.04.006
51030711 84200 4 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2086690 84200 4 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
73354931 96971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccc(S(C)(=O)=O)cc3)cn1)C2 10.1016/j.bmcl.2013.04.006
CHEMBL2382409 96971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccc(S(C)(=O)=O)cc3)cn1)C2 10.1016/j.bmcl.2013.04.006
51030984 84197 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2086687 84197 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 436 5 0 8 2.5 C[C@@H]1CN(C(=O)OCC(F)(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
51029601 84164 3 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086650 84164 3 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
73351961 96979 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2382417 96979 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 432 6 0 10 2.7 CC(C)c1nc(N2C3CCC2CN(c2ncc(OCc4ccncc4C#N)cn2)C3)no1 10.1016/j.bmcl.2013.04.006
155544367 180153 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at human GPR119 expressed in human HEK293 cells assessed as inhibition in agonist-induced beta-arrestin 2 recruitment incubated for 30 mins followed by agonist addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human GPR119 expressed in human HEK293 cells assessed as inhibition in agonist-induced beta-arrestin 2 recruitment incubated for 30 mins followed by agonist addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 508 3 0 4 6.0 CC[C@]12CCCN(C(=O)c3cccc(Br)c3)CCc3c(n(c4ccccc34)C(=O)C1)[C@@H]2OC 10.1021/acs.jmedchem.9b01924
CHEMBL4527708 180153 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at human GPR119 expressed in human HEK293 cells assessed as inhibition in agonist-induced beta-arrestin 2 recruitment incubated for 30 mins followed by agonist addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human GPR119 expressed in human HEK293 cells assessed as inhibition in agonist-induced beta-arrestin 2 recruitment incubated for 30 mins followed by agonist addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 508 3 0 4 6.0 CC[C@]12CCCN(C(=O)c3cccc(Br)c3)CCc3c(n(c4ccccc34)C(=O)C1)[C@@H]2OC 10.1021/acs.jmedchem.9b01924
51030985 96976 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382414 96976 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 5 0 8 2.1 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OCC(F)(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
73354931 96971 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccc(S(C)(=O)=O)cc3)cn1)C2 10.1016/j.bmcl.2013.04.006
CHEMBL2382409 96971 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccc(S(C)(=O)=O)cc3)cn1)C2 10.1016/j.bmcl.2013.04.006
51030053 84191 1 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086680 84191 1 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 396 4 0 8 2.4 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccncc3C#N)cn2)CC1 10.1016/j.bmcl.2013.04.006
51029601 84164 3 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
CHEMBL2086650 84164 3 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.5 CC(C)(C)OC(=O)N1CCN(c2ncc(OCc3ccc(S(C)(=O)=O)cc3)cn2)CC1 10.1016/j.bmcl.2013.04.006
51030711 84200 4 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
CHEMBL2086690 84200 4 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 420 6 0 10 2.5 CC(C)c1nc(N2CCN(c3ncc(OCc4ccncc4C#N)cn3)[C@H](C)C2)no1 10.1016/j.bmcl.2013.04.006
73353419 96974 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382412 96974 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
73348866 96975 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 492 5 0 8 3.2 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OC2CC(F)(F)C2(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382413 96975 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 492 5 0 8 3.2 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OC2CC(F)(F)C2(F)F)nc1 10.1016/j.bmcl.2013.04.006
73353419 96974 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382412 96974 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 480 5 0 8 3.0 C[C@@H]1CN(C(=O)OC2CC(F)(F)C2(F)F)CCN1c1ncc(OCc2ccncc2C#N)cn1 10.1016/j.bmcl.2013.04.006
73354930 96970 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1CC2CCC(C1)N2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382408 96970 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1CC2CCC(C1)N2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
72188621 96973 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382411 96973 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 466 5 0 8 2.6 N#Cc1cnccc1COc1cnc(N2CCN(C(=O)OC3CC(F)(F)C3(F)F)CC2)nc1 10.1016/j.bmcl.2013.04.006
73353420 96977 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382415 96977 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 448 5 0 8 2.7 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OCC(F)(F)F)nc1 10.1016/j.bmcl.2013.04.006
73348866 96975 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 492 5 0 8 3.2 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OC2CC(F)(F)C2(F)F)nc1 10.1016/j.bmcl.2013.04.006
CHEMBL2382413 96975 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 492 5 0 8 3.2 N#Cc1cnccc1COc1cnc(N2CC3CCC(C2)N3C(=O)OC2CC(F)(F)C2(F)F)nc1 10.1016/j.bmcl.2013.04.006
73350444 96972 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 4 0 8 2.9 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1016/j.bmcl.2013.04.006
CHEMBL2382410 96972 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from mouse GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 422 4 0 8 2.9 CC(C)(C)OC(=O)N1C2CCC1CN(c1ncc(OCc3ccncc3C#N)cn1)C2 10.1016/j.bmcl.2013.04.006
73354930 96970 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1CC2CCC(C1)N2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
CHEMBL2382408 96970 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysisDisplacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis
ChEMBL 474 5 0 8 3.0 CC(C)(C)OC(=O)N1CC2CCC(C1)N2c1ncc(OCc2ccc(S(C)(=O)=O)cc2)cn1 10.1016/j.bmcl.2013.04.006
71547153 92962 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 497 5 0 7 4.1 Cc1c(Oc2ccc(C(=O)N(C)C)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312160 92962 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 497 5 0 7 4.1 Cc1c(Oc2ccc(C(=O)N(C)C)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
51354342 68032 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@@H]2[C@H]3CO[C@@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766202 68032 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@@H]2[C@H]3CO[C@@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
71546035 93009 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 449 5 0 7 4.4 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312505 93009 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 449 5 0 7 4.4 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
71717312 92912 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 489 4 0 9 4.3 Cc1c(Oc2ccc(-n3cncn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2311545 92912 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 489 4 0 9 4.3 Cc1c(Oc2ccc(-n3cncn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
54584353 68008 0 None -2 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None -2 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
71545700 93022 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 516 5 0 8 4.0 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312519 93022 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 516 5 0 8 4.0 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
71546853 93016 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 465 3 0 7 4.7 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312513 93016 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 465 3 0 7 4.7 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71545538 93032 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 449 4 0 7 4.5 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CCC2)c1C 10.1021/jm301626p
CHEMBL2312528 93032 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 449 4 0 7 4.5 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CCC2)c1C 10.1021/jm301626p
67950429 90448 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 456 7 0 11 2.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)nc1 10.1021/ml300296q
CHEMBL2204984 90448 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 456 7 0 11 2.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)nc1 10.1021/ml300296q
16036825 68007 0 None -6 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
CHEMBL1766081 68007 0 None -6 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
71545699 93021 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 504 5 0 8 3.8 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312518 93021 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 504 5 0 8 3.8 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71546200 93012 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 439 5 0 8 3.7 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312509 93012 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 439 5 0 8 3.7 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71547007 92959 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 506 5 0 10 3.6 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312158 92959 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 506 5 0 10 3.6 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
54583401 68009 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(OC2C3COC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766083 68009 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(OC2C3COC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
71546202 93014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 453 4 0 8 4.1 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312511 93014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 453 4 0 8 4.1 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71547006 92958 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 494 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312157 92958 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 494 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71546036 93010 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 451 4 0 7 4.7 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312506 93010 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 451 4 0 7 4.7 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71546034 93008 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.3 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312504 93008 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.3 CCc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71545378 93025 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 409 4 0 7 3.6 CCOC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
CHEMBL2312521 93025 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 409 4 0 7 3.6 CCOC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
54584353 68008 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
71546857 92957 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 490 4 0 10 3.7 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312156 92957 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 490 4 0 10 3.7 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71545377 93024 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 423 4 0 7 4.0 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)C)c1C 10.1021/jm301626p
CHEMBL2312520 93024 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 423 4 0 7 4.0 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)C)c1C 10.1021/jm301626p
51354343 68033 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3CO[C@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766203 68033 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 414 5 0 8 2.9 Cc1ncccc1Oc1ncnc(O[C@H]2[C@@H]3CO[C@H]2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
16036825 68007 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
CHEMBL1766081 68007 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 386 5 0 7 3.7 Cc1ncccc1Oc1ncnc(OC2CCN(C(=O)OC(C)C)CC2)c1C 10.1021/jm200003p
71545535 93029 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.3 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OCC(C)C)c1C 10.1021/jm301626p
CHEMBL2312525 93029 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.3 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OCC(C)C)c1C 10.1021/jm301626p
67607375 90447 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 448 6 0 10 2.6 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)CC1 10.1021/ml300296q
CHEMBL2204983 90447 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 448 6 0 10 2.6 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(-n5cnnn5)cc4)c3C#N)CC2)CC1 10.1021/ml300296q
71545536 93030 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.4 CC[C@@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
CHEMBL2312526 93030 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.4 CC[C@@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
71546854 93017 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 475 5 0 9 3.9 Cc1c(Oc2ccc(-n3ccnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312514 93017 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 475 5 0 9 3.9 Cc1c(Oc2ccc(-n3ccnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71546201 93013 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 451 5 0 8 3.9 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312510 93013 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 451 5 0 8 3.9 COc1c(Oc2cccnc2C)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
54584353 68008 0 None -2 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None -2 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from rat GPR119 expressed in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
71716097 92963 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 507 4 0 9 4.4 Cc1c(Oc2ccc(-n3cncn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312161 92963 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 507 4 0 9 4.4 Cc1c(Oc2ccc(-n3cncn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
54584353 68008 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
CHEMBL1766082 68008 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation countingDisplacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 in human HEK293 cells by liquid scintillation counting
ChEMBL 428 5 0 8 3.2 Cc1ncccc1Oc1ncnc(OC2C3COCC2CN(C(=O)OC(C)C)C3)c1C 10.1021/jm200003p
67606673 90450 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 423 5 0 7 3.7 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)CC1 10.1021/ml300296q
CHEMBL2204986 90450 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 423 5 0 7 3.7 CC1(OC(=O)N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)CC1 10.1021/ml300296q
71545698 93020 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 518 4 0 8 4.2 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312517 93020 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 518 4 0 8 4.2 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71546856 93019 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 488 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
CHEMBL2312516 93019 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 488 5 0 10 3.4 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC1(C)CC1 10.1021/jm301626p
71545381 93028 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 3 0 7 4.4 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)(C)C)c1C 10.1021/jm301626p
CHEMBL2312524 93028 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 3 0 7 4.4 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)(C)C)c1C 10.1021/jm301626p
71545537 93031 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.4 CC[C@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
CHEMBL2312527 93031 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 437 5 0 7 4.4 CC[C@H](C)OC(=O)N1C2CC3CC1CC(C2)N3c1ncnc(Oc2cccnc2C)c1C 10.1021/jm301626p
71717324 93007 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 521 4 0 9 4.7 Cc1ncn(-c2ccc(Oc3ncnc(N4C5CC6CC4CC(C5)N6C(=O)OC(C)(C)C)c3C)c(F)c2)n1 10.1021/jm301626p
CHEMBL2312501 93007 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 521 4 0 9 4.7 Cc1ncn(-c2ccc(Oc3ncnc(N4C5CC6CC4CC(C5)N6C(=O)OC(C)(C)C)c3C)c(F)c2)n1 10.1021/jm301626p
11503692 77598 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1021/jm301626p
CHEMBL1951011 77598 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 467 6 0 8 3.5 Cc1c(Oc2ccc(S(C)(=O)=O)cc2F)ncnc1OC1CCN(C(=O)OC(C)C)CC1 10.1021/jm301626p
71545379 93026 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CC2)c1C 10.1021/jm301626p
CHEMBL2312522 93026 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2(C)CC2)c1C 10.1021/jm301626p
71545380 93027 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2CCC2)c1C 10.1021/jm301626p
CHEMBL2312523 93027 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 435 4 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC2CCC2)c1C 10.1021/jm301626p
71547008 92960 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 508 4 0 10 3.8 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
CHEMBL2312159 92960 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 508 4 0 10 3.8 Cc1c(Oc2ccc(-n3cnnn3)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)(C)C 10.1021/jm301626p
71546199 93011 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 441 3 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)(C)C)c1F 10.1021/jm301626p
CHEMBL2312508 93011 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 441 3 0 7 4.2 Cc1ncccc1Oc1ncnc(N2C3CC4CC2CC(C3)N4C(=O)OC(C)(C)C)c1F 10.1021/jm301626p
67633261 90449 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 431 6 0 8 3.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)nc1 10.1021/ml300296q
CHEMBL2204985 90449 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 431 6 0 8 3.5 CCc1cnc(N2CCC(n3ncc(COc4ccc(C#N)cc4F)c3C#N)CC2)nc1 10.1021/ml300296q
71546701 93015 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 451 4 0 7 4.3 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312512 93015 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 451 4 0 7 4.3 Cc1c(Oc2ccc(C#N)cc2F)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71546855 93018 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 476 5 0 10 3.3 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
CHEMBL2312515 93018 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 476 5 0 10 3.3 Cc1c(Oc2ccc(-n3cnnn3)cc2)ncnc1N1C2CC3CC1CC(C2)N3C(=O)OC(C)C 10.1021/jm301626p
71719746 92964 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 503 4 0 9 4.6 Cc1ncn(-c2ccc(Oc3ncnc(N4C5CC6CC4CC(C5)N6C(=O)OC(C)(C)C)c3C)cc2)n1 10.1021/jm301626p
CHEMBL2312162 92964 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assayBinding affinity to human GPR119 in HEK293FT cell membrane by radioligand binding assay
ChEMBL 503 4 0 9 4.6 Cc1ncn(-c2ccc(Oc3ncnc(N4C5CC6CC4CC(C5)N6C(=O)OC(C)(C)C)c3C)cc2)n1 10.1021/jm301626p
58114293 90446 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q
CHEMBL2204982 90446 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human GPR119Binding affinity to human GPR119
ChEMBL 480 6 0 10 3.0 Cn1nnnc1-c1ccc(OCc2cnn(C3CCN(C(=O)OC4(C)CC4)CC3)c2C#N)c(F)c1 10.1021/ml300296q