Ligand source activities (1 row/activity)





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5493324 105678 24 None 208 3 Human 10.8 pEC50 = 10.8 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279260 105678 24 None 208 3 Human 10.8 pEC50 = 10.8 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
24936626 24181 0 None 173 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257555 24181 0 None 173 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
44565931 19217 0 None 40 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186040 19217 0 None 40 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL446806 19217 0 None 40 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
44565931 19217 0 None 40 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186040 19217 0 None 40 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL446806 19217 0 None 40 4 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
24895263 201329 0 None 1122 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 10 4 6 4.6 Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)O)c(OC4CCCCC4)c3)cc2)cn1 10.1021/jm8000345
CHEMBL529659 201329 0 None 1122 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 10 4 6 4.6 Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)O)c(OC4CCCCC4)c3)cc2)cn1 10.1021/jm8000345
44591508 185774 0 None 1122 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 475 10 4 6 4.6 Nc1ccncc1[C@@H](O)CNCCc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1 10.1021/jm9000709
CHEMBL470857 185774 0 None 1122 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 475 10 4 6 4.6 Nc1ccncc1[C@@H](O)CNCCc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1 10.1021/jm9000709
76332894 112705 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 466 6 4 6 3.9 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccc(F)c3)N2)cc1 10.1021/jm4017224
CHEMBL3128199 112705 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 466 6 4 6 3.9 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccc(F)c3)N2)cc1 10.1021/jm4017224
24937389 24220 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 520 10 3 9 4.2 COCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257675 24220 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 520 10 3 9 4.2 COCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
24895363 180370 0 None 3162 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 11 3 4 5.3 CC(C)COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453322 180370 0 None 3162 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 11 3 4 5.3 CC(C)COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24894202 195804 0 None 676 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 473 10 3 4 6.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
CHEMBL509156 195804 0 None 676 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 473 10 3 4 6.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
45271036 202007 0 None 2951 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL550871 202007 0 None 2951 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
16223251 183238 0 None 204 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 6 3.9 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459646 183238 0 None 204 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 6 3.9 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
76336500 112700 0 None 2 4 Rhesus macaque 10.2 pEC50 = 10.2 Functional
Agonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128194 112700 0 None 2 4 Rhesus macaque 10.2 pEC50 = 10.2 Functional
Agonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
5493324 105678 24 None 208 3 Human 10.2 pEC50 = 10.2 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279260 105678 24 None 208 3 Human 10.2 pEC50 = 10.2 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
24895669 197446 0 None 7079 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 5 4.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL518168 197446 0 None 7079 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 5 4.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639494 19238 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 4 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
CHEMBL1186167 19238 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 4 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
CHEMBL452696 19238 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 4 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
23661589 100196 0 None 12589 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1cccc(-c2sccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245873 100196 0 None 12589 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1cccc(-c2sccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
42639656 202471 0 None 5 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL452134 202471 0 None 5 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL556852 202471 0 None 5 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
44560793 195676 0 None 7 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL507506 195676 0 None 7 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
16222940 193253 0 None 48 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL487682 193253 0 None 48 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44591507 186138 0 None 48 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473702 186138 0 None 48 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
44560794 180280 0 None 346 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 474 10 3 5 5.4 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
CHEMBL453056 180280 0 None 346 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 474 10 3 5 5.4 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
44565932 193790 0 None 4897 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 528 11 4 8 3.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL490733 193790 0 None 4897 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 528 11 4 8 3.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
24895361 192153 0 None 2 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL486051 192153 0 None 2 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
567 7512 16 None -2 7 Human 10.0 pEC50 = 10.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
9841972 7512 16 None -2 7 Human 10.0 pEC50 = 10.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
CHEMBL284782 7512 16 None -2 7 Human 10.0 pEC50 = 10.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
44560792 180167 0 None 794 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 3 5 4.5 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452798 180167 0 None 794 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 3 5 4.5 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
9845282 82727 0 None 63 3 Human 10.0 pEC50 = 10 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL205224 82727 0 None 63 3 Human 10.0 pEC50 = 10 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
11575154 83990 0 None 100000 2 Human 10.0 pEC50 = 10 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1ccncc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
CHEMBL207943 83990 0 None 100000 2 Human 10.0 pEC50 = 10 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1ccncc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
45271886 202094 0 None 724 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 508 11 3 5 4.5 CC(C)Cc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL551532 202094 0 None 724 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 508 11 3 5 4.5 CC(C)Cc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
6916441 106103 1 None 79 3 Human 10.0 pEC50 = 10.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL282190 106103 1 None 79 3 Human 10.0 pEC50 = 10.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
11156916 19282 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186550 19282 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL469395 19282 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
44565908 193903 0 None 75 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491726 193903 0 None 75 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
76332895 112706 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 466 6 4 6 3.9 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccc(F)cc3)N2)cc1 10.1021/jm4017224
CHEMBL3128200 112706 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 466 6 4 6 3.9 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccc(F)cc3)N2)cc1 10.1021/jm4017224
11272641 19215 0 None 10 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186009 19215 0 None 10 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL445481 19215 0 None 10 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
24936885 24255 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 9 3 8 4.6 CCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257797 24255 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 9 3 8 4.6 CCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
11224220 179746 0 None 2137 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 431 10 3 3 5.5 CC(C)Cc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL451760 179746 0 None 2137 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 431 10 3 3 5.5 CC(C)Cc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
10003858 195874 1 None 3548 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 10 4 5 4.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL510100 195874 1 None 3548 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 10 4 5 4.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11398536 19247 0 None 6309 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 535 11 4 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
CHEMBL1186241 19247 0 None 6309 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 535 11 4 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
CHEMBL455773 19247 0 None 6309 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 535 11 4 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
44565908 193903 0 None 75 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491726 193903 0 None 75 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
76336500 112700 0 None -2 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128194 112700 0 None -2 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
76336501 112704 0 None 56234 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 482 6 4 6 4.4 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccc(Cl)c3)N2)cc1 10.1021/jm4017224
CHEMBL3128198 112704 0 None 56234 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 482 6 4 6 4.4 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccc(Cl)c3)N2)cc1 10.1021/jm4017224
11268355 103171 0 None -1 3 Human 9.8 pEC50 = 9.8 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL26183 103171 0 None -1 3 Human 9.8 pEC50 = 9.8 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
45101537 202053 0 None 6 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL551272 202053 0 None 6 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
24895565 183474 0 None 575 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 11 3 5 5.5 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL459862 183474 0 None 575 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 11 3 5 5.5 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
44472636 112695 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 436 7 4 6 3.9 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
CHEMBL3128189 112695 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 436 7 4 6 3.9 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
24895265 193472 0 None 70 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
CHEMBL488430 193472 0 None 70 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
76336500 112700 0 None -3 4 Dog 9.7 pEC50 = 9.7 Functional
Agonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128194 112700 0 None -3 4 Dog 9.7 pEC50 = 9.7 Functional
Agonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
24895361 192153 0 None -2 3 Dog 9.7 pEC50 = 9.7 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL486051 192153 0 None -2 3 Dog 9.7 pEC50 = 9.7 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895357 193074 0 None 194 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 10 3 4 5.7 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL487443 193074 0 None 194 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 10 3 4 5.7 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895261 193443 0 None 676 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL488223 193443 0 None 676 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639654 19412 0 None 1258 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187156 19412 0 None 1258 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491891 19412 0 None 1258 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44591506 186111 0 None 676 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473495 186111 0 None 676 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
11669967 83295 0 None 12589 2 Human 9.7 pEC50 = 9.7 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 468 10 5 5 4.5 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL206002 83295 0 None 12589 2 Human 9.7 pEC50 = 9.7 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 468 10 5 5 4.5 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
42640122 202954 0 None 2 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL492401 202954 0 None 2 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL561335 202954 0 None 2 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
42639969 19344 0 None 1584 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 4 7 3.1 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186809 19344 0 None 1584 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 4 7 3.1 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL479530 19344 0 None 1584 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 4 7 3.1 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
76322047 112702 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 462 6 4 6 4.2 Nc1nc2c(s1)CCC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128196 112702 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 462 6 4 6 4.2 Nc1nc2c(s1)CCC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
24895557 179879 0 None 575 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 12 3 5 5.2 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452033 179879 0 None 575 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 12 3 5 5.2 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
24894323 183237 0 None 52 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 468 12 4 5 5.2 CCCOc1cc(-c2ccc(NCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459645 183237 0 None 52 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 468 12 4 5 5.2 CCCOc1cc(-c2ccc(NCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
11432806 72971 0 None 134 3 Human 9.7 pEC50 = 9.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
11432806 72971 0 None 134 3 Human 9.7 pEC50 = 9.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL184407 72971 0 None 134 3 Human 9.7 pEC50 = 9.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL184407 72971 0 None 134 3 Human 9.7 pEC50 = 9.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
16223045 202704 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 594 12 4 8 4.0 CC(=O)Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)NS(C)(=O)=O)c(OC4CCCCC4)c3)cc2)cn1 10.1016/j.bmcl.2009.06.083
CHEMBL559334 202704 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 594 12 4 8 4.0 CC(=O)Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)NS(C)(=O)=O)c(OC4CCCCC4)c3)cc2)cn1 10.1016/j.bmcl.2009.06.083
11647543 145014 0 None 2511 3 Human 9.6 pEC50 = 9.6 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL377028 145014 0 None 2511 3 Human 9.6 pEC50 = 9.6 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
9888047 100156 0 None 398 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245673 100156 0 None 398 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
24893964 193444 0 None 5 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL488224 193444 0 None 5 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
45268516 203022 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 605 13 5 9 2.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL561743 203022 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 605 13 5 9 2.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
24893964 193444 0 None 5 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL488224 193444 0 None 5 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
24895259 196075 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 528 12 5 7 3.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL512147 196075 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 528 12 5 7 3.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
11235459 199359 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 418 10 3 4 4.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL521406 199359 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 418 10 3 4 4.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24893964 193444 0 None 5 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL488224 193444 0 None 5 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
11235459 199359 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 3 4 4.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL521406 199359 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 3 4 4.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44396715 74225 0 None 20 3 Human 9.6 pEC50 = 9.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL189081 74225 0 None 20 3 Human 9.6 pEC50 = 9.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
24895561 183632 0 None 194 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 509 11 3 5 6.1 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL461301 183632 0 None 194 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 509 11 3 5 6.1 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
44396531 73609 0 None 38 3 Human 9.6 pEC50 = 9.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL186135 73609 0 None 38 3 Human 9.6 pEC50 = 9.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
24823464 104394 0 None 588 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL270964 104394 0 None 588 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
42640120 19348 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 507 10 3 6 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1C1CCCC1 10.1021/jm9000709
CHEMBL1186818 19348 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 507 10 3 6 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1C1CCCC1 10.1021/jm9000709
CHEMBL479727 19348 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 507 10 3 6 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1C1CCCC1 10.1021/jm9000709
24823464 104394 0 None 588 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL270964 104394 0 None 588 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
24823294 165847 0 None 870 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
CHEMBL409718 165847 0 None 870 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
24823294 165847 0 None 870 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL409718 165847 0 None 870 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
24895789 195646 0 None 72 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 375 8 3 3 4.3 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
CHEMBL507003 195646 0 None 72 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 375 8 3 3 4.3 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
24823294 165847 0 None 870 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL409718 165847 0 None 870 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
24895791 193419 0 None 199 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL488051 193419 0 None 199 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44396729 73636 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(N)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL186247 73636 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(N)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44441234 100564 0 None 63 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1ccc(-c2occc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247520 100564 0 None 63 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1ccc(-c2occc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
24895559 179880 0 None 338 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 483 12 3 5 5.4 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452034 179880 0 None 338 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 483 12 3 5 5.4 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
11352782 19289 0 None 2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 3 6 4.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186583 19289 0 None 2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 3 6 4.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL470856 19289 0 None 2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 3 6 4.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
42639652 19503 0 None 1513 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 3 6 3.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187716 19503 0 None 1513 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 3 6 3.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL516209 19503 0 None 1513 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 3 6 3.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
42639487 19298 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 520 10 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCCC1 10.1021/jm9000709
CHEMBL1186604 19298 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 520 10 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCCC1 10.1021/jm9000709
CHEMBL472293 19298 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 520 10 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCCC1 10.1021/jm9000709
24823296 104808 0 None 2884 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm701324c
CHEMBL273006 104808 0 None 2884 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm701324c
24823296 104808 0 None 2884 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
CHEMBL273006 104808 0 None 2884 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
16222840 202510 0 None 316 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 11 4 7 4.7 C[C@H](NCCc1ccc(-c2ccc(C(=O)NS(C)(=O)=O)c(OC3CCCCC3)c2)cc1)[C@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2009.06.083
CHEMBL557253 202510 0 None 316 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 11 4 7 4.7 C[C@H](NCCc1ccc(-c2ccc(C(=O)NS(C)(=O)=O)c(OC3CCCCC3)c2)cc1)[C@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2009.06.083
11268355 103171 0 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL26183 103171 0 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
9927453 103462 0 None 1 3 Human 9.4 pEC50 = 9.4 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL26393 103462 0 None 1 3 Human 9.4 pEC50 = 9.4 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
76336502 112707 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 449 6 4 7 3.2 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
CHEMBL3128201 112707 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 449 6 4 7 3.2 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
24949720 196301 0 None 66 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1 10.1021/jm800222k
CHEMBL514102 196301 0 None 66 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1 10.1021/jm800222k
42639314 19342 0 None 575 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
CHEMBL1186804 19342 0 None 575 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
CHEMBL479341 19342 0 None 575 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
44441235 157771 0 None 251 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1ccc(-c2sccc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL395834 157771 0 None 251 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1ccc(-c2sccc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
42639317 19485 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 506 10 3 5 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCC1 10.1021/jm9000709
CHEMBL1187617 19485 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 506 10 3 5 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCC1 10.1021/jm9000709
CHEMBL511968 19485 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 506 10 3 5 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCC1 10.1021/jm9000709
3931 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00571-x
9829836 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00571-x
CHEMBL12998 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00571-x
11224275 180273 0 None 1621 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 11 3 4 5.1 CCCOc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453048 180273 0 None 1621 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 11 3 4 5.1 CCCOc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11156916 19282 0 None 3 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186550 19282 0 None 3 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL469395 19282 0 None 3 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
3038500 16112 12 None 2 6 Rhesus macaque 9.4 pEC50 = 9.4 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 16112 12 None 2 6 Rhesus macaque 9.4 pEC50 = 9.4 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
3931 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00170-x
9829836 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00170-x
CHEMBL12998 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00170-x
3931 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00381-3
9829836 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00381-3
CHEMBL12998 9028 48 None 691 4 Human 9.4 pEC50 = 9.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00381-3
24822817 102070 0 None 120 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
CHEMBL256418 102070 0 None 120 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
24822817 102070 0 None 120 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL256418 102070 0 None 120 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
11340895 19287 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 494 11 3 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186563 19287 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 494 11 3 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL469821 19287 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 494 11 3 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
24822817 102070 0 None 120 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL256418 102070 0 None 120 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
44396798 176171 0 None 27 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL442225 176171 0 None 27 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
76329232 112685 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 447 6 3 5 4.5 Cc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128179 112685 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 447 6 3 5 4.5 Cc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
127041869 143884 0 None 27542 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 448 7 2 5 3.0 CCOC(=O)[C@@H]1[C@H]2CN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)C[C@H]21 10.1016/j.bmcl.2015.11.030
CHEMBL3747546 143884 0 None 27542 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 448 7 2 5 3.0 CCOC(=O)[C@@H]1[C@H]2CN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)C[C@H]21 10.1016/j.bmcl.2015.11.030
44560791 195875 0 None 154 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 376 8 3 4 3.7 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
CHEMBL510102 195875 0 None 154 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 376 8 3 4 3.7 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
24936882 24354 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 512 9 4 10 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258143 24354 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 512 9 4 10 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
42639656 202471 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
CHEMBL452134 202471 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
CHEMBL556852 202471 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
24894315 179752 0 None 165 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 11 3 5 5.2 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL451772 179752 0 None 165 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 11 3 5 5.2 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639491 19343 0 None 1659 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 3 6 5.3 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1SC1CCCCC1 10.1021/jm9000709
CHEMBL1186805 19343 0 None 1659 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 3 6 5.3 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1SC1CCCCC1 10.1021/jm9000709
CHEMBL479342 19343 0 None 1659 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 3 6 5.3 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1SC1CCCCC1 10.1021/jm9000709
42639656 202471 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL452134 202471 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL556852 202471 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
10113837 72343 0 None 39 2 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 435 11 5 5 3.3 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183129 72343 0 None 39 2 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 435 11 5 5 3.3 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44560793 195676 0 None -7 3 Dog 9.3 pEC50 = 9.3 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL507506 195676 0 None -7 3 Dog 9.3 pEC50 = 9.3 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44396513 73497 0 None 30 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL185660 73497 0 None 30 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
145984584 172666 0 None 5 3 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 444 10 5 4 4.4 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4249564 172666 0 None 5 3 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 444 10 5 4 4.4 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
24822819 167056 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 451 10 3 3 5.8 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL411028 167056 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 451 10 3 3 5.8 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
42639965 19490 0 None 691 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 534 11 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1CC1CCCCC1 10.1021/jm9000709
CHEMBL1187643 19490 0 None 691 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 534 11 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1CC1CCCCC1 10.1021/jm9000709
CHEMBL513419 19490 0 None 691 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 534 11 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1CC1CCCCC1 10.1021/jm9000709
44392552 71300 0 None 23 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181440 71300 0 None 23 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
24893966 183518 0 None 724 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 12 3 5 4.8 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL460257 183518 0 None 724 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 12 3 5 4.8 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44396596 130078 0 None 25 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL361505 130078 0 None 25 3 Human 9.3 pEC50 = 9.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
11453340 104516 0 None 2 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 435 10 3 4 5.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL271574 104516 0 None 2 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 435 10 3 4 5.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
11453340 104516 0 None 2 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 3 4 5.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL271574 104516 0 None 2 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 3 4 5.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
10100 10759 30 None -1 4 Rhesus macaque 9.2 pEC50 = 9.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None -1 4 Rhesus macaque 9.2 pEC50 = 9.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None -1 4 Rhesus macaque 9.2 pEC50 = 9.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None -1 4 Rhesus macaque 9.2 pEC50 = 9.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None -1 4 Rhesus macaque 9.2 pEC50 = 9.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
24822815 104718 0 None 588 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 467 11 3 4 5.6 CC(C)COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272583 104718 0 None 588 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 467 11 3 4 5.6 CC(C)COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
44396530 73862 0 None 23 3 Human 9.2 pEC50 = 9.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL187317 73862 0 None 23 3 Human 9.2 pEC50 = 9.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
10002049 104217 0 None 3 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL270026 104217 0 None 3 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
10002049 104217 0 None 3 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL270026 104217 0 None 3 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639810 19283 0 None 4 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 530 11 3 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
CHEMBL1186551 19283 0 None 4 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 530 11 3 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
CHEMBL469396 19283 0 None 4 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 530 11 3 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
11420551 19291 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186589 19291 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL471060 19291 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10002049 104217 0 None 3 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL270026 104217 0 None 3 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44472633 144717 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 443 6 3 5 3.4 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2cccc(=O)n21 10.1021/acs.jmedchem.5b01372
CHEMBL3763934 144717 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 443 6 3 5 3.4 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2cccc(=O)n21 10.1021/acs.jmedchem.5b01372
24822648 104383 0 None 28 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
CHEMBL270889 104383 0 None 28 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
24936881 24289 0 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257913 24289 0 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
42639808 19297 0 None 1230 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 522 11 3 6 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCC1 10.1021/jm9000709
CHEMBL1186601 19297 0 None 1230 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 522 11 3 6 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCC1 10.1021/jm9000709
CHEMBL472090 19297 0 None 1230 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 522 11 3 6 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCC1 10.1021/jm9000709
11156916 19282 0 None -3 2 Dog 9.2 pEC50 = 9.2 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186550 19282 0 None -3 2 Dog 9.2 pEC50 = 9.2 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL469395 19282 0 None -3 2 Dog 9.2 pEC50 = 9.2 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
42639133 19498 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187691 19498 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL515397 19498 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
51347436 112683 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 433 6 3 5 4.2 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
CHEMBL3128177 112683 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 433 6 3 5 4.2 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
44396736 73642 0 None 11 3 Human 9.2 pEC50 = 9.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL186271 73642 0 None 11 3 Human 9.2 pEC50 = 9.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44298804 204209 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 483 11 5 7 2.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc2c(c1)CCN2 10.1016/s0960-894x(99)00277-2
CHEMBL56968 204209 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 483 11 5 7 2.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc2c(c1)CCN2 10.1016/s0960-894x(99)00277-2
9906822 168816 0 None -3 3 Human 9.2 pEC50 = 9.2 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL416012 168816 0 None -3 3 Human 9.2 pEC50 = 9.2 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
44472637 112696 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 436 7 4 6 3.9 C[C@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
CHEMBL3128190 112696 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 436 7 4 6 3.9 C[C@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
11352782 19289 0 None -2 2 Dog 9.2 pEC50 = 9.2 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 3 6 4.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186583 19289 0 None -2 2 Dog 9.2 pEC50 = 9.2 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 3 6 4.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL470856 19289 0 None -2 2 Dog 9.2 pEC50 = 9.2 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 3 6 4.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
24894317 180479 0 None 22 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 11 3 4 5.6 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453575 180479 0 None 22 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 11 3 4 5.6 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44565907 199949 0 None 138 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 498 11 4 8 2.3 CCOc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL523149 199949 0 None 138 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 498 11 4 8 2.3 CCOc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
24949728 182019 0 None 436 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 479 8 3 4 5.7 CC(C)Oc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
CHEMBL457199 182019 0 None 436 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 479 8 3 4 5.7 CC(C)Oc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
24895664 183475 0 None 251 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 12 3 4 5.8 CCCOc1cc(-c2ccc(CCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459863 183475 0 None 251 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 12 3 4 5.8 CCCOc1cc(-c2ccc(CCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44268556 30907 0 None 354 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 515 12 5 8 2.9 COC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13389 30907 0 None 354 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 515 12 5 8 2.9 COC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44298731 204860 0 None 870 3 Human 9.1 pEC50 = 9.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 429 10 2 3 4.9 CCCCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL57430 204860 0 None 870 3 Human 9.1 pEC50 = 9.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 429 10 2 3 4.9 CCCCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44396577 73726 0 None 25 3 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL186676 73726 0 None 25 3 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
10075383 103880 0 None 229 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 520 11 4 6 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL267545 103880 0 None 229 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 520 11 4 6 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00169-3
24950234 182776 0 None 223 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 4 5 5.8 CCCNc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL458923 182776 0 None 223 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 4 5 5.8 CCCNc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
24950716 182319 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 4.9 COc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
CHEMBL457847 182319 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 4.9 COc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
24950236 195851 0 None 89 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 9 4 5 6.8 O=C(O)c1cc(NC2CCCCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL509729 195851 0 None 89 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 9 4 5 6.8 O=C(O)c1cc(NC2CCCCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
24950562 181906 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 401 6 3 3 4.5 Cc1ccc([C@@H](O)CN[C@H]2CCc3ccc(-c4ccc(C(=O)O)cc4)cc3C2)cc1 10.1021/jm800222k
CHEMBL456971 181906 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 401 6 3 3 4.5 Cc1ccc([C@@H](O)CN[C@H]2CCc3ccc(-c4ccc(C(=O)O)cc4)cc3C2)cc1 10.1021/jm800222k
24895359 199273 0 None 104 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 405 9 3 4 4.3 COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL520903 199273 0 None 104 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 405 9 3 4 4.3 COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11060184 126508 0 None 39 3 Human 9.1 pEC50 = 9.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 11 4 6 3.5 C[C@H](CNc1ccc(CC(=O)NS(=O)(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL347616 126508 0 None 39 3 Human 9.1 pEC50 = 9.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 11 4 6 3.5 C[C@H](CNc1ccc(CC(=O)NS(=O)(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
44441229 100524 0 None 100 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2nc(C(=O)O)cs2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247315 100524 0 None 100 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2nc(C(=O)O)cs2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
10298567 72727 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1cccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmcl.2004.11.001
CHEMBL183611 72727 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1cccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmcl.2004.11.001
44298787 201528 0 None 426 3 Human 9.1 pEC50 = 9.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 12 2 5 6.6 CCCCCCCCc1csc(Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL53679 201528 0 None 426 3 Human 9.1 pEC50 = 9.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 12 2 5 6.6 CCCCCCCCc1csc(Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
24823292 165673 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 433 11 3 4 5.0 CC(C)COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL409533 165673 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 433 11 3 4 5.0 CC(C)COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
24950570 182209 0 None 794 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1F 10.1021/jm800222k
CHEMBL457629 182209 0 None 794 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1F 10.1021/jm800222k
11476004 180272 0 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453047 180272 0 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
45267631 202722 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 12 4 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(C[C@@H](CO)NC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
CHEMBL559486 202722 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 12 4 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(C[C@@H](CO)NC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
11156916 19282 0 None -3 2 Dog 9.1 pEC50 = 9.1 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186550 19282 0 None -3 2 Dog 9.1 pEC50 = 9.1 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL469395 19282 0 None -3 2 Dog 9.1 pEC50 = 9.1 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 536 11 3 6 4.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
76318364 112697 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 450 8 4 6 4.3 CC[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
CHEMBL3128191 112697 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 450 8 4 6 4.3 CC[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
24950568 196544 0 None 234 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1 10.1021/jm800222k
CHEMBL516002 196544 0 None 234 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1 10.1021/jm800222k
44396779 73835 0 None 17 3 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL187209 73835 0 None 17 3 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
11340895 19287 0 None -1 2 Dog 9.1 pEC50 = 9.1 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 494 11 3 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186563 19287 0 None -1 2 Dog 9.1 pEC50 = 9.1 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 494 11 3 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL469821 19287 0 None -1 2 Dog 9.1 pEC50 = 9.1 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 494 11 3 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
76325669 112698 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 464 9 4 6 4.6 CCC[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
CHEMBL3128192 112698 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 464 9 4 6 4.6 CCC[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
44396532 73530 0 None 42 3 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185836 73530 0 None 42 3 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44472590 65435 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1021/acs.jmedchem.5b01372
CHEMBL1684585 65435 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1021/acs.jmedchem.5b01372
44298288 108360 0 None 575 3 Human 9.1 pEC50 = 9.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 441 9 1 5 5.8 CCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL298594 108360 0 None 575 3 Human 9.1 pEC50 = 9.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 441 9 1 5 5.8 CCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
24895365 180371 0 None 309 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 10 3 4 5.5 CC(C)Oc1cc(-c2ccc(CC(C)(C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453323 180371 0 None 309 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 10 3 4 5.5 CC(C)Oc1cc(-c2ccc(CC(C)(C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11373418 106305 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 416 9 3 5 3.6 COC(=O)COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL283426 106305 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 416 9 3 5 3.6 COC(=O)COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
44298533 201783 0 None 1380 3 Human 9.0 pEC50 = 9.0 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 469 11 1 5 6.5 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL54821 201783 0 None 1380 3 Human 9.0 pEC50 = 9.0 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 469 11 1 5 6.5 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
9929683 118088 0 None 3548 2 Rat 9.0 pEC50 = 9.0 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32670 118088 0 None 3548 2 Rat 9.0 pEC50 = 9.0 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44396675 134035 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 543 11 4 7 3.2 COc1cccc(S(=O)(=O)Nc2cccc([C@@H](O)CNCCc3c[nH]c4c(S(C)(=O)=O)cccc34)c2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL365833 134035 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 543 11 4 7 3.2 COc1cccc(S(=O)(=O)Nc2cccc([C@@H](O)CNCCc3c[nH]c4c(S(C)(=O)=O)cccc34)c2)c1 10.1016/j.bmcl.2004.09.054
11199616 106792 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 372 8 3 3 4.5 CCOc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL286819 106792 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 372 8 3 3 4.5 CCOc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
1499 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
3779 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
536 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
CHEMBL434 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
DB01064 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
1499 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
3779 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
536 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
CHEMBL434 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
DB01064 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
1499 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
3779 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
536 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
CHEMBL434 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
DB01064 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
1499 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
3779 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
536 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
CHEMBL434 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
DB01064 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
1499 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
3779 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
536 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
CHEMBL434 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
DB01064 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
11324939 101238 1 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25133 101238 1 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
1499 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
3779 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
536 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
CHEMBL434 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
DB01064 8872 47 None -190 38 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
44472590 65435 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1021/jm4017224
CHEMBL1684585 65435 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1021/jm4017224
44472590 65435 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2015.11.030
CHEMBL1684585 65435 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2015.11.030
44472590 65435 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2010.12.087
CHEMBL1684585 65435 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 422 7 4 6 3.3 Nc1nc(CC(=O)Nc2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2010.12.087
24823127 104719 0 None 1 3 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272584 104719 0 None 1 3 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
45101537 202053 0 None -6 3 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at dog recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL551272 202053 0 None -6 3 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at dog recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
42639133 19498 0 None -1 2 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187691 19498 0 None -1 2 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL515397 19498 0 None -1 2 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
42639656 202471 0 None -5 2 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL452134 202471 0 None -5 2 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL556852 202471 0 None -5 2 Dog 9.0 pEC50 = 9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
24949568 196462 0 None 338 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 536 9 4 6 5.6 O=C(O)c1cc(NC2CCOCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL515349 196462 0 None 338 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 536 9 4 6 5.6 O=C(O)c1cc(NC2CCOCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
24936492 24321 0 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258026 24321 0 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
42639967 19284 0 None 128 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186557 19284 0 None 128 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL469610 19284 0 None 128 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44268520 28011 0 None 128 3 Human 9.0 pEC50 = 9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 591 14 5 8 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)OCc1ccccc1 10.1016/s0960-894x(98)00170-x
CHEMBL13132 28011 0 None 128 3 Human 9.0 pEC50 = 9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 591 14 5 8 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)OCc1ccccc1 10.1016/s0960-894x(98)00170-x
44268495 31802 0 None 151 3 Human 9.0 pEC50 = 9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 612 19 6 7 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13467 31802 0 None 151 3 Human 9.0 pEC50 = 9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 612 19 6 7 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44392175 138572 0 None -1 2 Human 9.0 pEC50 = 9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 480 12 5 7 3.2 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2004.11.001
CHEMBL369346 138572 0 None -1 2 Human 9.0 pEC50 = 9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 480 12 5 7 3.2 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2004.11.001
11785699 71614 0 None 12 2 Human 9.0 pEC50 = 9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 519 12 4 6 4.9 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC/C=C/c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182018 71614 0 None 12 2 Human 9.0 pEC50 = 9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 519 12 4 6 4.9 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC/C=C/c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44396559 73622 0 None 7 2 Human 9.0 pEC50 = 9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 499 11 4 6 4.7 CCOc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL186196 73622 0 None 7 2 Human 9.0 pEC50 = 9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 499 11 4 6 4.7 CCOc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
44396625 130849 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 547 10 4 6 3.9 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(Cl)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL363246 130849 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 547 10 4 6 3.9 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(Cl)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44386369 175275 0 None - 1 Human 9.0 pEC50 = 9 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 629 10 4 10 3.2 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(N5CCCCC5)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL435307 175275 0 None - 1 Human 9.0 pEC50 = 9 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 629 10 4 10 3.2 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(N5CCCCC5)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
10283539 174644 0 None 346 3 Human 9.0 pEC50 = 9 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 697 14 6 9 2.8 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00607-8
CHEMBL431048 174644 0 None 346 3 Human 9.0 pEC50 = 9 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 697 14 6 9 2.8 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00607-8
44298851 107330 0 None 63 3 Human 9.0 pEC50 = 9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 463 11 1 4 6.5 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL291467 107330 0 None 63 3 Human 9.0 pEC50 = 9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 463 11 1 4 6.5 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
10189730 12049 0 None 426 2 Human 9.0 pEC50 = 9 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 647 14 6 8 3.4 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
CHEMBL106511 12049 0 None 426 2 Human 9.0 pEC50 = 9 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 647 14 6 8 3.4 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
3931 9028 48 None 691 4 Human 9.0 pEC50 = 9 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
9829836 9028 48 None 691 4 Human 9.0 pEC50 = 9 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
CHEMBL12998 9028 48 None 691 4 Human 9.0 pEC50 = 9 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
145983603 172592 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 410 10 5 4 3.3 CC(C)NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4248369 172592 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 410 10 5 4 3.3 CC(C)NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
145985242 172324 0 None 6 3 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 443 11 4 4 3.9 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4241613 172324 0 None 6 3 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 443 11 4 4 3.9 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
11420551 19291 0 None -1 3 Dog 9.0 pEC50 = 9.0 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186589 19291 0 None -1 3 Dog 9.0 pEC50 = 9.0 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL471060 19291 0 None -1 3 Dog 9.0 pEC50 = 9.0 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
567 7512 16 None -2 7 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.11.060
9841972 7512 16 None -2 7 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.11.060
CHEMBL284782 7512 16 None -2 7 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.11.060
10100 10759 30 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
24823127 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272584 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
24823127 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL272584 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1016/j.bmcl.2008.08.009
24823127 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL272584 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
24823127 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL272584 104719 0 None -1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
44268534 26136 0 None 199 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 529 13 5 8 3.3 CCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL12911 26136 0 None 199 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 529 13 5 8 3.3 CCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268605 105190 0 None 489 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 542 14 6 7 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL275511 105190 0 None 489 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 542 14 6 7 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44392181 72845 0 None 10 2 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccccc1NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183744 72845 0 None 10 2 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccccc1NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44396738 130662 0 None 54 3 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 655 13 5 9 4.8 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccc(C(=O)O)cc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL362763 130662 0 None 54 3 Human 9.0 pEC50 = 9.0 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 655 13 5 9 4.8 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccc(C(=O)O)cc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
76322044 112686 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 3 6 3.9 Cc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
CHEMBL3128180 112686 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 3 6 3.9 Cc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
44565931 19217 0 None -40 4 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186040 19217 0 None -40 4 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL446806 19217 0 None -40 4 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
11453340 104516 0 None -2 2 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 3 4 5.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL271574 104516 0 None -2 2 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 3 4 5.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
52943770 24139 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 492 8 4 9 3.8 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257438 24139 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 492 8 4 9 3.8 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
45270197 202175 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(N)c3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
CHEMBL552012 202175 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 551 11 4 7 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(N)c3)cc2)cc1OC1CCCCC1 10.1016/j.bmcl.2009.06.083
24895563 183517 0 None 173 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 12 3 5 4.5 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL460256 183517 0 None 173 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 12 3 5 4.5 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44268539 27199 0 None 371 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 527 13 5 7 3.4 CC(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13068 27199 0 None 371 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 527 13 5 7 3.4 CC(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268496 105151 0 None 125 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 542 13 6 7 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL275291 105151 0 None 125 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 542 13 6 7 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
213051 99354 2 None 4 2 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24350 99354 2 None 4 2 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
44392457 172736 0 None 34 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL425161 172736 0 None 34 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44396737 73632 0 None 6 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 683 14 4 10 5.2 CCOC(=O)c1ccc(S(=O)(=O)Oc2cccc3c(C[C@@H](C)NC[C@H](O)c4cccc(NS(=O)(=O)c5cccs5)c4)c[nH]c23)cc1 10.1016/j.bmcl.2004.10.035
CHEMBL186236 73632 0 None 6 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 683 14 4 10 5.2 CCOC(=O)c1ccc(S(=O)(=O)Oc2cccc3c(C[C@@H](C)NC[C@H](O)c4cccc(NS(=O)(=O)c5cccs5)c4)c[nH]c23)cc1 10.1016/j.bmcl.2004.10.035
44402732 140403 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 653 17 3 6 8.2 CCCCCCc1ccc(-c2csc(Cc3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5ccccc5)cc4)cc3)n2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL371427 140403 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 653 17 3 6 8.2 CCCCCCc1ccc(-c2csc(Cc3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5ccccc5)cc4)cc3)n2)cc1 10.1016/j.bmcl.2005.03.119
44298852 108520 0 None 117 3 Human 8.9 pEC50 = 8.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL299719 108520 0 None 117 3 Human 8.9 pEC50 = 8.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
44301617 205494 0 None 43651 3 Human 8.9 pEC50 = 8.9 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 640 16 3 7 7.7 CCCCCCc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL58241 205494 0 None 43651 3 Human 8.9 pEC50 = 8.9 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 640 16 3 7 7.7 CCCCCCc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
11134054 53757 0 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 444 10 4 6 4.1 C[C@H](CNc1ccc(CC(=O)Nc2nccs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154150 53757 0 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 444 10 4 6 4.1 C[C@H](CNc1ccc(CC(=O)Nc2nccs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
10346448 126608 0 None 501 3 Human 8.9 pEC50 = 8.9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348501 126608 0 None 501 3 Human 8.9 pEC50 = 8.9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
44565931 19217 0 None -40 4 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186040 19217 0 None -40 4 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL446806 19217 0 None -40 4 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
24893964 193444 0 None -5 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL488224 193444 0 None -5 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
44441236 100198 0 None 3162 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 416 9 4 5 4.5 O=C(O)c1ccsc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245875 100198 0 None 3162 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 416 9 4 5 4.5 O=C(O)c1ccsc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
44441232 100563 0 None 19 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2ocnc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247519 100563 0 None 19 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2ocnc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44268268 25423 1 None 186 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 493 11 4 7 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00169-3
CHEMBL12769 25423 1 None 186 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 493 11 4 7 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00169-3
24893964 193444 0 None -5 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL488224 193444 0 None -5 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
24893964 193444 0 None -5 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL488224 193444 0 None -5 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
24949566 181651 1 None 281 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 8 4 5 5.0 CC(=O)Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL456353 181651 1 None 281 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 8 4 5 5.0 CC(=O)Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
76336500 112700 0 None -21 4 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128194 112700 0 None -21 4 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
44396488 73505 0 None 5 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 556 12 4 7 3.8 C[C@H](Cc1c[nH]c2c(OCC(=O)N(C)C)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185703 73505 0 None 5 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 556 12 4 7 3.8 C[C@H](Cc1c[nH]c2c(OCC(=O)N(C)C)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44268268 25423 1 None 186 3 Human 8.9 pEC50 = 8.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 493 11 4 7 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00381-3
CHEMBL12769 25423 1 None 186 3 Human 8.9 pEC50 = 8.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 493 11 4 7 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00381-3
44298823 108056 0 None 1174 3 Human 8.9 pEC50 = 8.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 462 11 1 3 7.1 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
CHEMBL296380 108056 0 None 1174 3 Human 8.9 pEC50 = 8.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 462 11 1 3 7.1 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
76322043 112684 0 None 1 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
CHEMBL3128178 112684 0 None 1 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
44335548 116542 0 None 288 3 Human 8.9 pEC50 = 8.9 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 567 17 5 6 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL323113 116542 0 None 288 3 Human 8.9 pEC50 = 8.9 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 567 17 5 6 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
11272641 19215 0 None -10 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186009 19215 0 None -10 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL445481 19215 0 None -10 3 Dog 8.9 pEC50 = 8.9 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
76322043 112684 0 None 1 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/acs.jmedchem.5b01372
CHEMBL3128178 112684 0 None 1 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/acs.jmedchem.5b01372
24949883 182874 0 None 691 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c(F)c1 10.1021/jm800222k
CHEMBL459133 182874 0 None 691 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c(F)c1 10.1021/jm800222k
42639489 19309 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 12 3 6 4.4 CCCSc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186640 19309 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 12 3 6 4.4 CCCSc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL473493 19309 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 12 3 6 4.4 CCCSc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44268509 26193 0 None 154 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 513 13 5 7 3.1 CCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL12943 26193 0 None 154 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 513 13 5 7 3.1 CCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268632 30999 0 None 245 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 514 12 6 7 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13398 30999 0 None 245 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 514 12 6 7 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268563 103960 0 None 162 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 569 17 5 7 4.7 CCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL268289 103960 0 None 162 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 569 17 5 7 4.7 CCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
145983164 172719 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 517 11 6 6 4.6 COC(=O)Nc1ccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4250902 172719 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 517 11 6 6 4.6 COC(=O)Nc1ccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)cc1 10.1016/j.ejmech.2018.03.032
145986105 172149 0 None 25 3 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 429 10 4 4 4.0 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4237453 172149 0 None 25 3 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 429 10 4 4 4.0 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
24949891 194947 0 None 46 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
CHEMBL498703 194947 0 None 46 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
145983745 172272 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 474 11 5 5 4.4 COc1ccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4240360 172272 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 474 11 5 5 4.4 COc1ccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)cc1 10.1016/j.ejmech.2018.03.032
24895783 185713 0 None 6 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL470292 185713 0 None 6 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895783 185713 0 None 6 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL470292 185713 0 None 6 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44392230 72371 1 None -1 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 479 12 6 6 3.0 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2004.11.001
CHEMBL183283 72371 1 None -1 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 479 12 6 6 3.0 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2004.11.001
11124502 126486 0 None 630 2 Human 8.8 pEC50 = 8.8 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 551 13 4 7 3.3 C[C@H](CNc1cccc(CCS(=O)(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL347400 126486 0 None 630 2 Human 8.8 pEC50 = 8.8 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 551 13 4 7 3.3 C[C@H](CNc1cccc(CCS(=O)(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
9823696 82550 0 None 398 3 Human 8.8 pEC50 = 8.8 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.7 Cc1ccc(C(=O)O)cc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
CHEMBL204827 82550 0 None 398 3 Human 8.8 pEC50 = 8.8 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.7 Cc1ccc(C(=O)O)cc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
44441230 100562 0 None 7 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2csc(C(=O)O)n2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247518 100562 0 None 7 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2csc(C(=O)O)n2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
24895783 185713 0 None 6 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL470292 185713 0 None 6 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44335534 11598 0 None 100 3 Human 8.8 pEC50 = 8.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 559 13 5 6 4.1 O=C(NCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104193 11598 0 None 100 3 Human 8.8 pEC50 = 8.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 559 13 5 6 4.1 O=C(NCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
16118894 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00169-3
3467 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00169-3
CHEMBL276257 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00169-3
44580040 193899 0 None 2 3 Dog 8.8 pEC50 = 8.8 Functional
Agonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 510 10 4 5 5.7 CC(C)(C)C(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL491645 193899 0 None 2 3 Dog 8.8 pEC50 = 8.8 Functional
Agonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 510 10 4 5 5.7 CC(C)(C)C(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
10100 10759 30 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
76336499 112699 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 464 8 4 6 4.5 CC(C)[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
CHEMBL3128193 112699 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 464 8 4 6 4.5 CC(C)[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1csc(N)n1 10.1021/jm4017224
24936489 24290 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257914 24290 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
44377754 126728 0 None 478 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 589 14 3 8 4.7 O=c1n(CCCC2CCCC2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL349651 126728 0 None 478 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 589 14 3 8 4.7 O=c1n(CCCC2CCCC2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44392212 175148 0 None -12 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL1204383 175148 0 None -12 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL434524 175148 0 None -12 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
16118894 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00381-3
3467 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00381-3
CHEMBL276257 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00381-3
44298843 203442 0 None 151 3 Human 8.8 pEC50 = 8.8 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1ccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)nc1 10.1016/s0960-894x(99)00277-2
CHEMBL56449 203442 0 None 151 3 Human 8.8 pEC50 = 8.8 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1ccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)nc1 10.1016/s0960-894x(99)00277-2
145984044 172455 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 517 11 6 6 4.6 COC(=O)Nc1cccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4244932 172455 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 517 11 6 6 4.6 COC(=O)Nc1cccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)c1 10.1016/j.ejmech.2018.03.032
11221652 101855 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 344 6 4 3 3.8 CC(Cc1c[nH]c2c(O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25534 101855 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 344 6 4 3 3.8 CC(Cc1c[nH]c2c(O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
11187476 102077 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NCC(O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL25645 102077 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NCC(O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
67972107 143870 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 444 6 2 6 3.0 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1C[C@H]2[C@@H](C1)[C@@H]2c1nnco1 10.1016/j.bmcl.2015.11.030
CHEMBL3747356 143870 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 444 6 2 6 3.0 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1C[C@H]2[C@@H](C1)[C@@H]2c1nnco1 10.1016/j.bmcl.2015.11.030
44472591 144799 0 None 1288 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 468 7 3 6 3.4 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764774 144799 0 None 1288 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 468 7 3 6 3.4 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
24937014 24180 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257554 24180 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52946357 24494 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258598 24494 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
44396568 74060 0 None 34 3 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL188196 74060 0 None 34 3 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44396659 74138 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188622 74138 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44298850 174962 0 None 263 3 Human 8.8 pEC50 = 8.8 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 461 8 1 4 6.1 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL433252 174962 0 None 263 3 Human 8.8 pEC50 = 8.8 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 461 8 1 4 6.1 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)n1 10.1016/s0960-894x(99)00277-2
65772 67177 8 None 2 11 Human 8.8 pEC50 = 8.8 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL174984 67177 8 None 2 11 Human 8.8 pEC50 = 8.8 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
145984040 172442 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 573 15 6 6 6.1 CCCCCOC(=O)Nc1cccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4244608 172442 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 573 15 6 6 6.1 CCCCCOC(=O)Nc1cccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)c1 10.1016/j.ejmech.2018.03.032
10092953 104811 0 None 34 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
CHEMBL273028 104811 0 None 34 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
24950401 183804 0 None 147 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 481 8 3 6 4.5 CN(C)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL463181 183804 0 None 147 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 481 8 3 6 4.5 CN(C)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
24949726 196319 0 None 457 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
CHEMBL514265 196319 0 None 457 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
44298849 203231 0 None 251 3 Human 8.7 pEC50 = 8.7 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 434 9 1 3 6.3 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
CHEMBL56308 203231 0 None 251 3 Human 8.7 pEC50 = 8.7 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 434 9 1 3 6.3 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
76332893 112703 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 476 6 4 6 4.6 Nc1nc2c(s1)CCCC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128197 112703 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 476 6 4 6 4.6 Nc1nc2c(s1)CCCC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
44579941 190890 0 None 3 2 Dog 8.7 pEC50 = 8.7 Functional
Agonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 3 5 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1N1CCCC1=O 10.1016/j.bmcl.2008.08.009
CHEMBL482627 190890 0 None 3 2 Dog 8.7 pEC50 = 8.7 Functional
Agonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 3 5 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1N1CCCC1=O 10.1016/j.bmcl.2008.08.009
127041558 143795 0 None 5754 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 476 5 2 5 4.0 CC1(C)CC2(CCN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)CC2)C(=O)O1 10.1016/j.bmcl.2015.11.030
CHEMBL3746280 143795 0 None 5754 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 476 5 2 5 4.0 CC1(C)CC2(CCN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)CC2)C(=O)O1 10.1016/j.bmcl.2015.11.030
44579651 193935 0 None 14 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.1 C[C@H](Cc1cccc(Oc2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.08.009
CHEMBL492006 193935 0 None 14 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.1 C[C@H](Cc1cccc(Oc2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.08.009
44268571 31403 0 None 138 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 582 13 6 7 4.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)NC1CCCCC1 10.1016/s0960-894x(98)00170-x
CHEMBL13432 31403 0 None 138 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 582 13 6 7 4.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)NC1CCCCC1 10.1016/s0960-894x(98)00170-x
46881871 14926 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 411 9 4 7 2.7 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1csc(N)n1 10.1016/j.bmcl.2010.01.130
CHEMBL1091816 14926 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 411 9 4 7 2.7 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1csc(N)n1 10.1016/j.bmcl.2010.01.130
76325667 112687 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 461 7 3 5 4.8 CCc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128181 112687 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 461 7 3 5 4.8 CCc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
44441231 154833 0 None 50 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393470 154833 0 None 50 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
10940242 171977 0 None 31 3 Human 8.0 pEC50 = 8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 12 4 6 3.8 C[C@H](CNc1ccc(CCS(=O)(=O)NC(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL422876 171977 0 None 31 3 Human 8.0 pEC50 = 8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 12 4 6 3.8 C[C@H](CNc1ccc(CCS(=O)(=O)NC(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
213051 99354 2 None 4 2 Human 8.0 pEC50 = 8 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24350 99354 2 None 4 2 Human 8.0 pEC50 = 8 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
10160869 19882 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 446 9 3 5 3.1 CC1CCN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL1190409 19882 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 446 9 3 5 3.1 CC1CCN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL540816 19882 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 446 9 3 5 3.1 CC1CCN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
24895783 185713 0 None -6 2 Dog 8.0 pEC50 = 8 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL470292 185713 0 None -6 2 Dog 8.0 pEC50 = 8 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44565908 193903 0 None -75 3 Dog 8.0 pEC50 = 8 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491726 193903 0 None -75 3 Dog 8.0 pEC50 = 8 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10239722 119235 0 None -44 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 119235 0 None -44 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
24949416 194767 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 8 3 4 4.7 O=C(O)COc1cccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL497281 194767 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 8 3 4 4.7 O=C(O)COc1cccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
52948056 24291 0 None -1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257915 24291 0 None -1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
44268498 105123 0 None 12 3 Human 8.0 pEC50 = 8 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 612 17 4 7 4.8 CCCCCCN(C)C(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL275114 105123 0 None 12 3 Human 8.0 pEC50 = 8 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 612 17 4 7 4.8 CCCCCCN(C)C(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
9871800 63262 0 None 120 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
CHEMBL163262 63262 0 None 120 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
46882030 12540 0 None 39 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 427 9 4 5 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ncc[nH]2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078576 12540 0 None 39 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 427 9 4 5 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ncc[nH]2)c1 10.1016/j.bmcl.2010.01.130
46881840 15180 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.3 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
CHEMBL1093385 15180 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.3 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
CHEMBL1204416 15180 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.3 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
44392575 71146 0 None 2 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181300 71146 0 None 2 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
9871800 63262 0 None 120 3 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity as cAMP accumulation in CHO cellsBeta 3-adrenergic receptor agonistic activity as cAMP accumulation in CHO cells
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL163262 63262 0 None 120 3 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity as cAMP accumulation in CHO cellsBeta 3-adrenergic receptor agonistic activity as cAMP accumulation in CHO cells
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
12147227 68766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
142109147 68766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44386630 68766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
69921317 68766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
CHEMBL177442 68766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
135995978 135254 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 556 8 5 10 2.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NC#N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL366657 135254 0 None - 1 Human 8.0 pEC50 = 8 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 556 8 5 10 2.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NC#N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
44331425 11217 0 None 100 3 Human 8.0 pEC50 = 8 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
CHEMBL101630 11217 0 None 100 3 Human 8.0 pEC50 = 8 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
44313161 110552 0 None 100 3 Human 8.0 pEC50 = 8 Functional
Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nMCompound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308860 110552 0 None 100 3 Human 8.0 pEC50 = 8 Functional
Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nMCompound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
44402821 76736 0 None - 1 Human 8.0 pEC50 = 8 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 605 18 3 6 7.3 CCCCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
CHEMBL193944 76736 0 None - 1 Human 8.0 pEC50 = 8 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 605 18 3 6 7.3 CCCCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
10121514 11020 0 None - 1 Human 8.0 pEC50 = 8 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 602 15 6 8 3.4 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100458 11020 0 None - 1 Human 8.0 pEC50 = 8 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 602 15 6 8 3.4 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(02)00607-8
44301832 207854 1 None 301 3 Human 8.0 pEC50 = 8 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 592 17 3 7 6.8 CCCCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL60281 207854 1 None 301 3 Human 8.0 pEC50 = 8 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 592 17 3 7 6.8 CCCCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
44281424 107082 0 None 245 3 Human 8.0 pEC50 = 8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 587 12 3 9 4.2 O=C(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL289249 107082 0 None 245 3 Human 8.0 pEC50 = 8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 587 12 3 9 4.2 O=C(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
44281408 120091 0 None 263 3 Human 8.0 pEC50 = 8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 646 13 4 10 4.4 COC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL33155 120091 0 None 263 3 Human 8.0 pEC50 = 8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 646 13 4 10 4.4 COC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
12049924 210576 0 None 69 3 Human 8.0 pEC50 = 8 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 606 13 3 9 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL68301 210576 0 None 69 3 Human 8.0 pEC50 = 8 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 606 13 3 9 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
16126657 143964 0 None 2 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 573 14 4 8 4.2 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL374867 143964 0 None 2 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 573 14 4 8 4.2 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCC3)c12 10.1016/j.bmcl.2006.08.010
145983042 172376 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 573 15 6 6 6.1 CCCCCOC(=O)Nc1ccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4242824 172376 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 573 15 6 6 6.1 CCCCCOC(=O)Nc1ccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)cc1 10.1016/j.ejmech.2018.03.032
10209243 174553 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 544 11 4 7 4.1 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CCCC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL430392 174553 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 544 11 4 7 4.1 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CCCC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
10475645 115721 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 392 9 4 5 2.8 C[C@H](NCCc1ccc(N(C)CC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32115 115721 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 392 9 4 5 2.8 C[C@H](NCCc1ccc(N(C)CC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44335560 12087 0 None 19 3 Human 7.0 pEC50 = 7 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 469 10 5 6 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL106746 12087 0 None 19 3 Human 7.0 pEC50 = 7 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 469 10 5 6 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
53357711 71272 0 None -100 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814279 71272 0 None -100 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814280 71272 0 None -100 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
9871096 73424 0 None -158 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814268 73424 0 None -158 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1852860 73424 0 None -158 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
24824228 167307 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 411 9 3 4 4.7 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL411234 167307 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 411 9 3 4 4.7 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
56672271 73315 0 None -398 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835859 73315 0 None -398 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852407 73315 0 None -398 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
1499 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
45268136 203164 0 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203989 203164 0 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL562669 203164 0 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
44517692 203448 0 None -14 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203990 203448 0 None -14 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL564516 203448 0 None -14 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
24824228 167307 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2008.08.009
CHEMBL411234 167307 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2008.08.009
1499 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
3779 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
536 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
CHEMBL434 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
DB01064 8872 47 None -190 38 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
52948805 24527 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 502 9 2 7 5.5 CC(C)c1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258704 24527 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 502 9 2 7 5.5 CC(C)c1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
44461468 112405 0 None 30 3 Human 7.0 pEC50 = 7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 608 17 4 9 3.7 CCCCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL312364 112405 0 None 30 3 Human 7.0 pEC50 = 7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 608 17 4 9 3.7 CCCCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44461485 113720 0 None 85 2 Human 7.0 pEC50 = 7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 564 15 3 9 3.7 CCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL314893 113720 0 None 85 2 Human 7.0 pEC50 = 7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 564 15 3 9 3.7 CCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44392499 133927 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 542 11 3 7 3.7 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(CS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL365669 133927 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 542 11 3 7 3.7 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(CS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44268253 24865 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 331 9 3 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12679 24865 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 331 9 3 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
2419 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
559 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
CHEMBL1263 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
DB00938 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
1499 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
2419 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 10236 84 None -416 14 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
1499 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/S0960-894X(96)00603-8
3779 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/S0960-894X(96)00603-8
536 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/S0960-894X(96)00603-8
CHEMBL434 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/S0960-894X(96)00603-8
DB01064 8872 47 None -190 38 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/S0960-894X(96)00603-8
44311370 210931 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 317 9 3 5 2.0 COc1ccc(CCNC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL70557 210931 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 317 9 3 5 2.0 COc1ccc(CCNC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/S0960-894X(96)00603-8
12578 7723 61 None -186 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
2755 7723 61 None -186 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
CHEMBL1374751 7723 61 None -186 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
123686 8762 51 None -12302 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
12581 8762 51 None -12302 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
CHEMBL11268 8762 51 None -12302 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
5311116 9114 9 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
544 9114 9 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
CHEMBL207802 9114 9 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
66653268 95026 0 None -3311 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
CHEMBL2348201 95026 0 None -3311 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
56598967 95036 0 None -2238 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
CHEMBL2348211 95036 0 None -2238 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
56598833 95042 0 None -436 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
CHEMBL2348217 95042 0 None -436 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
56598832 95043 0 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 95043 0 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
56597179 95044 0 None -2754 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348219 95044 0 None -2754 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
56598831 95918 0 None -1023 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348220 95918 0 None -1023 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2365796 95918 0 None -1023 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
1960 9632 67 None -1047 19 Rat 4.0 pEC50 = 4 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 9632 67 None -1047 19 Rat 4.0 pEC50 = 4 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 9632 67 None -1047 19 Rat 4.0 pEC50 = 4 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 9632 67 None -1047 19 Rat 4.0 pEC50 = 4 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 9632 67 None -1047 19 Rat 4.0 pEC50 = 4 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
155774 10868 40 None -2041 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2848 10868 40 None -2041 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
538 10868 40 None -2041 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
CHEMBL75753 10868 40 None -2041 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
DB13781 10868 40 None -2041 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
10186687 12193 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 528 15 4 4 6.2 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107270 12193 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 528 15 4 4 6.2 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)CC1 10.1016/s0960-894x(01)00645-x
46881616 14714 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 396 9 3 6 2.9 Cc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
CHEMBL1090424 14714 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 396 9 3 6 2.9 Cc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
46882084 12553 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(CCc2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078695 12553 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(CCc2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
44472610 144735 0 None -234 4 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764088 144735 0 None -234 4 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
11419142 100257 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 434 9 3 3 5.7 CC(Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24615 100257 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 434 9 3 3 5.7 CC(Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
10100 10759 30 None -4 4 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None -4 4 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None -4 4 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None -4 4 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None -4 4 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
24895783 185713 0 None -6 2 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL470292 185713 0 None -6 2 Dog 8.0 pEC50 = 8.0 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 420 10 3 5 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
53318280 65429 0 None 70 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 623 11 3 6 7.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684578 65429 0 None 70 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 623 11 3 6 7.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
44580010 193578 0 None 46 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 441 10 3 5 4.7 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL489199 193578 0 None 46 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 441 10 3 5 4.7 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44268464 26183 0 None 10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 585 17 5 8 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL12939 26183 0 None 10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 585 17 5 8 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
11270071 105766 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279931 105766 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
44392519 130570 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 493 11 4 6 4.4 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL362293 130570 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 493 11 4 6 4.4 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
10283146 114050 0 None 2 3 Human 8.0 pEC50 = 8.0 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 656 12 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(CC(=O)O)c5ccccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL317003 114050 0 None 2 3 Human 8.0 pEC50 = 8.0 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 656 12 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(CC(=O)O)c5ccccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
12017004 106932 0 None 426 3 Human 8.0 pEC50 = 8.0 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL287880 106932 0 None 426 3 Human 8.0 pEC50 = 8.0 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
44281407 107081 0 None 229 3 Human 8.0 pEC50 = 8.0 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 666 14 4 10 3.6 CS(=O)(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL289248 107081 0 None 229 3 Human 8.0 pEC50 = 8.0 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 666 14 4 10 3.6 CS(=O)(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
12049925 105470 0 None 66 3 Human 8.0 pEC50 = 8.0 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 638 13 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL277613 105470 0 None 66 3 Human 8.0 pEC50 = 8.0 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 638 13 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
145983355 172580 0 None 26 3 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 454 12 3 5 3.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4248093 172580 0 None 26 3 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 454 12 3 5 3.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
44419254 89919 0 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 587 14 4 8 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCCC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL218210 89919 0 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 587 14 4 8 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCCC3)c12 10.1016/j.bmcl.2006.08.010
10028830 9026 40 None 323 3 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
3932 9026 40 None 323 3 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4238084 9026 40 None 323 3 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
44268352 22311 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 380 10 4 6 1.3 CS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12188 22311 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 380 10 4 6 1.3 CS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44127169 203082 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 422 11 4 7 1.9 O=C(Cc1ncccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL562154 203082 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 422 11 4 7 1.9 O=C(Cc1ncccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44311756 211449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 335 9 3 5 2.1 COc1ccc(CCNC[C@@H](O)COc2ccc(F)c(O)c2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL73770 211449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 335 9 3 5 2.1 COc1ccc(CCNC[C@@H](O)COc2ccc(F)c(O)c2)cc1 10.1016/S0960-894X(96)00603-8
44309305 108936 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 513 12 4 8 1.6 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)C2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL302597 108936 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 513 12 4 8 1.6 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)C2)cc1 10.1016/s0960-894x(03)00387-1
122184835 129319 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601310 129319 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
52943383 24353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 544 9 2 8 5.3 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258142 24353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 544 9 2 8 5.3 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2010.08.039
146015362 7734 10 None -891 5 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00063-4
3462 7734 10 None -891 5 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00063-4
5486546 7734 10 None -891 5 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00063-4
CHEMBL1204876 7734 10 None -891 5 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00063-4
44444363 100759 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 402 8 2 6 4.1 O[C@@H](CNCCc1ccc(-c2csc(-c3cccnc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL248560 100759 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 402 8 2 6 4.1 O[C@@H](CNCCc1ccc(-c2csc(-c3cccnc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
11324939 101238 1 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25133 101238 1 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
11221586 102257 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 342 6 3 2 4.4 Cc1ccc2c(CC(C)NCC(O)c3cccc(Cl)c3)c[nH]c2c1 10.1016/s0960-894x(03)00073-8
CHEMBL25724 102257 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 342 6 3 2 4.4 Cc1ccc2c(CC(C)NCC(O)c3cccc(Cl)c3)c[nH]c2c1 10.1016/s0960-894x(03)00073-8
44268249 26286 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 331 9 4 5 2.4 C[C@@H](CCc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12994 26286 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 331 9 4 5 2.4 C[C@@H](CCc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
44444154 162402 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 504 11 4 7 3.4 CC1C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
CHEMBL404626 162402 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 504 11 4 7 3.4 CC1C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
1499 8872 47 None -190 38 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
3779 8872 47 None -190 38 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
536 8872 47 None -190 38 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
CHEMBL434 8872 47 None -190 38 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
DB01064 8872 47 None -190 38 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
24823466 19603 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 440 11 4 5 4.4 O=C(O)COc1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL1188436 19603 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 440 11 4 5 4.4 O=C(O)COc1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL536330 19603 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 440 11 4 5 4.4 O=C(O)COc1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
24822972 104307 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(CCNC[C@H](O)c2cccc(Cl)c2)ccc1-c1ccc(C(=O)O)cc1 10.1021/jm701324c
CHEMBL270460 104307 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(CCNC[C@H](O)c2cccc(Cl)c2)ccc1-c1ccc(C(=O)O)cc1 10.1021/jm701324c
44579650 193934 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 10 4 6 3.4 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL492005 193934 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 10 4 6 3.4 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
127037832 144830 0 None -2 4 Rhesus macaque 7.9 pEC50 = 7.9 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None -2 4 Rhesus macaque 7.9 pEC50 = 7.9 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
11324939 101238 1 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptorAgonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptor
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25133 101238 1 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptorAgonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptor
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
10298968 64280 0 None 239 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 471 9 4 8 2.3 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL166085 64280 0 None 239 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 471 9 4 8 2.3 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44402688 140370 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 647 14 3 6 7.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(CCc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL371247 140370 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 647 14 3 6 7.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(CCc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44285634 107184 0 None 22 3 Human 7.9 pEC50 = 7.9 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 576 17 3 7 6.3 CCCCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL290131 107184 0 None 22 3 Human 7.9 pEC50 = 7.9 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 576 17 3 7 6.3 CCCCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
11342656 209438 0 None 165 3 Human 7.9 pEC50 = 7.9 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 634 13 3 7 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL61429 209438 0 None 165 3 Human 7.9 pEC50 = 7.9 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 634 13 3 7 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
15483880 106388 0 None 208 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL28405 106388 0 None 208 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
9938030 106801 0 None 138 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286859 106801 0 None 138 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44281469 106893 0 None 57 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL287561 106893 0 None 57 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44281097 121511 0 None 288 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33384 121511 0 None 288 3 Human 7.9 pEC50 = 7.9 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
44444169 161776 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 580 13 4 7 4.6 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(Cc1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL401335 161776 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 580 13 4 7 4.6 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(Cc1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.09.011
76318362 112689 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 474 7 3 6 4.5 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2sc(C3CC3)nc21 10.1021/jm4017224
CHEMBL3128183 112689 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 474 7 3 6 4.5 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2sc(C3CC3)nc21 10.1021/jm4017224
11810896 126260 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 375 9 4 4 3.1 CC(=O)NCc1ccc(NC[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm0101500
CHEMBL345304 126260 0 None -3 3 Human 7.9 pEC50 = 7.9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 375 9 4 4 3.1 CC(=O)NCc1ccc(NC[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm0101500
9871386 119048 5 None -56 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3290999 119048 5 None -56 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
90645345 119256 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 119256 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
90645346 119272 0 None -14 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 119272 0 None -14 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
56658405 73362 0 None -25 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1835856 73362 0 None -25 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1852565 73362 0 None -25 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
56668796 73376 0 None -39 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835860 73376 0 None -39 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852632 73376 0 None -39 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
9871386 119048 5 None -56 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290999 119048 5 None -56 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
11797099 117239 0 None 19 2 Rat 7.9 pEC50 = 7.9 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 434 11 4 5 3.7 C[C@H](NCCc1ccc(N(CC(=O)O)Cc2ccccc2)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32470 117239 0 None 19 2 Rat 7.9 pEC50 = 7.9 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 434 11 4 5 3.7 C[C@H](NCCc1ccc(N(CC(=O)O)Cc2ccccc2)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
11152564 106791 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL286818 106791 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
44280957 119328 0 None 251 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 590 13 3 9 3.4 O=C(CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1)N1CCCC1 10.1016/s0960-894x(00)00267-5
CHEMBL32996 119328 0 None 251 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 590 13 3 9 3.4 O=C(CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1)N1CCCC1 10.1016/s0960-894x(00)00267-5
44444378 101030 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3cccnc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250146 101030 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3cccnc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
2796082 13607 4 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1083995 13607 4 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
44574978 196069 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 524 12 2 6 4.0 O=C(Cc1nccn1Cc1ccccc1)N1CCCc2cc(CCNC[C@H](O)COc3ccccc3)ccc21 10.1016/j.bmc.2009.03.044
CHEMBL512099 196069 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 524 12 2 6 4.0 O=C(Cc1nccn1Cc1ccccc1)N1CCCc2cc(CCNC[C@H](O)COc3ccccc3)ccc21 10.1016/j.bmc.2009.03.044
44126931 202133 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 496 12 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL551831 202133 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 496 12 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
2796082 13607 4 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1083995 13607 4 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
9915920 209549 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 564 14 5 8 2.7 C[C@H](Cc1ccc(OCP(=O)(O)c2ccccc2)cc1)NC[C@H](O)COc1ccc(O)c(NS(C)(=O)=O)c1 10.1016/S0960-894X(96)00603-8
CHEMBL62091 209549 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 564 14 5 8 2.7 C[C@H](Cc1ccc(OCP(=O)(O)c2ccccc2)cc1)NC[C@H](O)COc1ccc(O)c(NS(C)(=O)=O)c1 10.1016/S0960-894X(96)00603-8
44309363 109417 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 559 8 4 8 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(S(=O)(=O)c3ccc4oc5ccccc5c4c3)CC2)ccc1O 10.1016/s0960-894x(03)00387-1
CHEMBL304346 109417 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 559 8 4 8 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(S(=O)(=O)c3ccc4oc5ccccc5c4c3)CC2)ccc1O 10.1016/s0960-894x(03)00387-1
10140428 210639 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 476 9 4 8 1.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL68685 210639 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 476 9 4 8 1.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(03)00387-1
44307113 176162 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 552 11 3 5 3.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL442172 176162 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 552 11 3 5 3.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
44127480 203336 0 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL563810 203336 0 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
45273268 202408 0 None -194 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204004 202408 0 None -194 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL556274 202408 0 None -194 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10100 10759 30 None -23 4 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None -23 4 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None -23 4 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None -23 4 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None -23 4 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
46881838 14709 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 393 9 3 6 2.4 Cc1cc(C)n(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
CHEMBL1090416 14709 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 393 9 3 6 2.4 Cc1cc(C)n(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
46833102 20978 0 None -79 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1084656 20978 0 None -79 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198882 20978 0 None -79 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
2419 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
5152 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
559 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
CHEMBL1263 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
DB00938 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
2419 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
5152 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
559 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
CHEMBL1263 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
DB00938 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
2419 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
5152 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
559 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
CHEMBL1263 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
DB00938 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
42625513 19331 0 None -2511 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL1186722 19331 0 None -2511 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL475389 19331 0 None -2511 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
2419 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
5152 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
559 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
CHEMBL1263 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
DB00938 10236 84 None -416 14 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
46832227 20969 2 None -5 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
CHEMBL1083884 20969 2 None -5 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
CHEMBL1198851 20969 2 None -5 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
10280222 11247 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 534 12 5 7 2.6 CC(C)CNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL101836 11247 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 534 12 5 7 2.6 CC(C)CNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
10076885 106560 0 None 208 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 577 14 3 9 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCOC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
CHEMBL285242 106560 0 None 208 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 577 14 3 9 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCOC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
44580009 193580 0 None 42 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.0 Cc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL489201 193580 0 None 42 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.0 Cc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
24949724 182507 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 388 6 3 4 3.6 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccnc2)CC3)cc1 10.1021/jm800222k
CHEMBL458271 182507 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 388 6 3 4 3.6 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccnc2)CC3)cc1 10.1021/jm800222k
45381932 129314 0 None 41 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 432 10 4 6 2.8 CC(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601305 129314 0 None 41 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 432 10 4 6 2.8 CC(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
10132882 101284 0 None 13 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat adrenergic beta-3 receptor assessed as cAMP productionAgonist activity at rat adrenergic beta-3 receptor assessed as cAMP production
ChEMBL 355 8 2 6 3.2 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL251599 101284 0 None 13 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat adrenergic beta-3 receptor assessed as cAMP productionAgonist activity at rat adrenergic beta-3 receptor assessed as cAMP production
ChEMBL 355 8 2 6 3.2 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
44377650 126983 0 None 389 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 577 13 3 6 4.6 O=C1N(CCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL351967 126983 0 None 389 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 577 13 3 6 4.6 O=C1N(CCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44461706 212702 0 None 154 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 579 15 3 7 4.1 CCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL84117 212702 0 None 154 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 579 15 3 7 4.1 CCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
11270069 102476 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25823 102476 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
9873257 91720 16 None 47 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22375 91720 16 None 47 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
44377535 62191 0 None 117 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 508 8 4 9 2.8 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4cccc5nc(O)ccc45)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL161949 62191 0 None 117 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 508 8 4 9 2.8 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4cccc5nc(O)ccc45)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44392190 72357 0 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 421 10 5 5 3.2 O=C(Nc1ccccc1)Nc1ccc(C[C@H](O)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183211 72357 0 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 421 10 5 5 3.2 O=C(Nc1ccccc1)Nc1ccc(C[C@H](O)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44396739 134023 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 471 10 4 6 3.9 COc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL365828 134023 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 471 10 4 6 3.9 COc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44306959 209862 0 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 520 11 4 7 2.8 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL63842 209862 0 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 520 11 4 7 2.8 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
9826638 210078 1 None 41 3 Human 7.9 pEC50 = 7.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 484 12 4 7 3.2 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64760 210078 1 None 41 3 Human 7.9 pEC50 = 7.9 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 484 12 4 7 3.2 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44298256 203891 0 None 4 3 Human 7.9 pEC50 = 7.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 426 9 1 6 4.7 CCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
CHEMBL56768 203891 0 None 4 3 Human 7.9 pEC50 = 7.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 426 9 1 6 4.7 CCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
1499 8872 47 None -338 38 Rat 7.9 pEC50 = 7.9 Functional
In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
3779 8872 47 None -338 38 Rat 7.9 pEC50 = 7.9 Functional
In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
536 8872 47 None -338 38 Rat 7.9 pEC50 = 7.9 Functional
In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
CHEMBL434 8872 47 None -338 38 Rat 7.9 pEC50 = 7.9 Functional
In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
DB01064 8872 47 None -338 38 Rat 7.9 pEC50 = 7.9 Functional
In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
76325668 112688 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 462 7 3 6 4.2 CCc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
CHEMBL3128182 112688 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 462 7 3 6 4.2 CCc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
44444166 101213 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 532 12 4 7 4.0 CC(C)C1C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
CHEMBL251176 101213 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 532 12 4 7 4.0 CC(C)C1C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
12043159 106789 0 None 446 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 14 3 9 3.7 CC(=O)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL286800 106789 0 None 446 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 14 3 9 3.7 CC(=O)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44444369 100879 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 479 10 3 6 4.3 CCc1nc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)c(NS(C)(=O)=O)c3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL249164 100879 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 479 10 3 6 4.3 CCc1nc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)c(NS(C)(=O)=O)c3)cc2)cs1 10.1016/j.bmcl.2007.06.072
44219629 185348 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1nccn1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467083 185348 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1nccn1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
44461567 110951 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 579 15 3 7 4.1 CCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL309673 110951 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 579 15 3 7 4.1 CCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
44461488 212154 0 None 776 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 606 13 3 7 3.0 O=C(CCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O)N1CCCC1 10.1016/s0960-894x(99)00072-4
CHEMBL79915 212154 0 None 776 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 606 13 3 7 3.0 O=C(CCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O)N1CCCC1 10.1016/s0960-894x(99)00072-4
10553603 106474 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 506 10 6 8 1.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(NC(=O)CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284612 106474 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 506 10 6 8 1.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(NC(=O)CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
53319639 65432 0 None 1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684582 65432 0 None 1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
10187653 11108 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 554 11 5 7 3.5 O=C(Nc1ccccc1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100970 11108 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 554 11 5 7 3.5 O=C(Nc1ccccc1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
24812046 161971 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@@H](Oc1ccc(CCNC[C@@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL402462 161971 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@@H](Oc1ccc(CCNC[C@@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
10203259 19906 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 434 10 3 6 2.2 CC1CCN(S(=O)(=O)Nc2ccc(OCCNC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL1190536 19906 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 434 10 3 6 2.2 CC1CCN(S(=O)(=O)Nc2ccc(OCCNC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL541072 19906 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 434 10 3 6 2.2 CC1CCN(S(=O)(=O)Nc2ccc(OCCNC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
44444356 160893 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 339 7 2 5 3.4 Cc1nc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL398515 160893 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 339 7 2 5 3.4 Cc1nc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
11349698 100964 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 386 9 3 3 4.9 CCCOc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL24967 100964 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 386 9 3 3 4.9 CCCOc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
44444167 101214 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 546 13 4 7 4.4 CC(C)CC1C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
CHEMBL251177 101214 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 546 13 4 7 4.4 CC(C)CC1C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
44579965 200034 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
CHEMBL523817 200034 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
45381852 129300 0 None 60 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601204 129300 0 None 60 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
10347866 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
10347866 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL22386 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
CHEMBL22386 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44461719 212643 0 None 630 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 641 14 3 6 5.0 O=C1N(CCCC(F)(F)C(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL83754 212643 0 None 630 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 641 14 3 6 5.0 O=C1N(CCCC(F)(F)C(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
10347866 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
CHEMBL22386 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
46881574 14555 0 None 218 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 3 6 2.9 O=C(Cn1cc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089386 14555 0 None 218 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 3 6 2.9 O=C(Cn1cc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
10347866 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00277-2
CHEMBL22386 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00277-2
10099346 147851 0 None 125 3 Human 7.9 pEC50 = 7.9 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38254 147851 0 None 125 3 Human 7.9 pEC50 = 7.9 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
10347866 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(00)00422-4
CHEMBL22386 91782 1 None 851 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(00)00422-4
12049920 109409 0 None 54 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL304298 109409 0 None 54 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
12049916 209773 0 None 91 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 576 11 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63138 209773 0 None 91 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 576 11 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
10483845 209851 0 None 1479 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 608 11 3 8 5.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63760 209851 0 None 1479 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 608 11 3 8 5.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
12049926 209861 0 None 43 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 654 14 3 10 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63825 209861 0 None 43 3 Human 7.9 pEC50 = 7.9 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 654 14 3 10 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
9844606 117100 0 None 1000 2 Rat 7.9 pEC50 = 7.9 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32391 117100 0 None 1000 2 Rat 7.9 pEC50 = 7.9 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44127678 203081 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1cc2ccccc2cn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL562153 203081 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1cc2ccccc2cn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
9896817 109662 0 None 22 3 Human 6.9 pEC50 = 6.9 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL305891 109662 0 None 22 3 Human 6.9 pEC50 = 6.9 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
45268128 203101 0 None -26 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203988 203101 0 None -26 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL562315 203101 0 None -26 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
46881870 14871 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 407 9 3 6 3.0 Cc1cc(C)n(C(C)C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
CHEMBL1091479 14871 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 407 9 3 6 3.0 Cc1cc(C)n(C(C)C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
10273529 20066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 418 10 4 5 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)NC1CCCCC1 10.1016/s0960-894x(04)00462-7
CHEMBL1191786 20066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 418 10 4 5 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)NC1CCCCC1 10.1016/s0960-894x(04)00462-7
CHEMBL542930 20066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 418 10 4 5 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)NC1CCCCC1 10.1016/s0960-894x(04)00462-7
44268274 25622 0 None 24 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cccc(Cl)c1 10.1016/s0960-894x(98)00169-3
CHEMBL12813 25622 0 None 24 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cccc(Cl)c1 10.1016/s0960-894x(98)00169-3
12043156 174928 0 None 63 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 575 14 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
CHEMBL433042 174928 0 None 63 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 575 14 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
53326195 65428 0 None 144 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684577 65428 0 None 144 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
24822472 104189 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL269920 104189 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
52947562 24459 0 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258486 24459 0 None -3 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
44377513 63284 0 None 131 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL163531 63284 0 None 131 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44392508 71995 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 494 11 3 6 4.3 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182614 71995 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 494 11 3 6 4.3 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
12017005 107045 0 None 131 3 Human 7.8 pEC50 = 7.8 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(CCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL288917 107045 0 None 131 3 Human 7.8 pEC50 = 7.8 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(CCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00277-8
10626150 106802 0 None 208 3 Human 7.8 pEC50 = 7.8 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 534 11 5 9 1.3 CCOC(=O)CNC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL286868 106802 0 None 208 3 Human 7.8 pEC50 = 7.8 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 534 11 5 9 1.3 CCOC(=O)CNC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
44281468 168661 0 None 131 3 Human 7.8 pEC50 = 7.8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 623 12 3 8 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL415039 168661 0 None 131 3 Human 7.8 pEC50 = 7.8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 623 12 3 8 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
9799092 54080 0 None 12 3 Human 7.8 pEC50 = 7.8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154419 54080 0 None 12 3 Human 7.8 pEC50 = 7.8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11038599 54642 0 None 15 3 Human 7.8 pEC50 = 7.8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 516 11 5 6 3.7 C[C@H](CNc1cccc(CNC(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154906 54642 0 None 15 3 Human 7.8 pEC50 = 7.8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 516 11 5 6 3.7 C[C@H](CNc1cccc(CNC(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
9799092 54080 0 None 12 3 Human 7.8 pEC50 = 7.8 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL154419 54080 0 None 12 3 Human 7.8 pEC50 = 7.8 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
9799092 54080 0 None 12 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL154419 54080 0 None 12 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441226 100443 0 None -1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL246908 100443 0 None -1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441227 154828 0 None 7 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393469 154828 0 None 7 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
56658407 73412 0 None -31 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835857 73412 0 None -31 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852796 73412 0 None -31 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
44335628 11608 0 None 66 3 Human 6.8 pEC50 = 6.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 498 12 4 7 3.7 CCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104222 11608 0 None 66 3 Human 6.8 pEC50 = 6.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 498 12 4 7 3.7 CCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
52947487 23938 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 587 12 1 9 4.8 OC(COc1ccccc1)CN(CCCN1CCOCC1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1256008 23938 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 587 12 1 9 4.8 OC(COc1ccccc1)CN(CCCN1CCOCC1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52948572 24072 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 488 9 0 7 5.4 COC(COc1ccccc1)CN(C)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257205 24072 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 488 9 0 7 5.4 COC(COc1ccccc1)CN(C)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52944896 24073 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 486 6 0 7 5.1 c1ccc(OCC2CN(C3CCN(c4ncnc5scc(-c6ccccc6)c45)CC3)CCO2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257206 24073 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 486 6 0 7 5.1 c1ccc(OCC2CN(C3CCN(c4ncnc5scc(-c6ccccc6)c45)CC3)CCO2)cc1 10.1016/j.bmcl.2010.08.039
52941935 24254 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 486 6 0 7 5.2 O=C1OC(COc2ccccc2)CN1C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257796 24254 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 486 6 0 7 5.2 O=C1OC(COc2ccccc2)CN1C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52943968 24566 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258824 24566 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
52941547 24568 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 10 2 8 4.1 OCCN(CC(O)COc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258826 24568 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 10 2 8 4.1 OCCN(CC(O)COc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52950121 24569 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 502 8 1 7 4.6 CC(=O)N(CC(O)COc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258827 24569 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 502 8 1 7 4.6 CC(=O)N(CC(O)COc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52947654 24598 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 474 8 1 7 4.7 CN(CC(O)COc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258941 24598 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 474 8 1 7 4.7 CN(CC(O)COc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52942807 24599 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 550 10 1 7 6.3 OC(COc1ccccc1)CN(Cc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258942 24599 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 550 10 1 7 6.3 OC(COc1ccccc1)CN(Cc1ccccc1)C1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
44268327 105075 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 448 11 4 6 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C1CCCCC1 10.1016/s0960-894x(98)00169-3
CHEMBL274807 105075 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 448 11 4 6 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C1CCCCC1 10.1016/s0960-894x(98)00169-3
44127167 203035 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1cccnc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561818 203035 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1cccnc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
9845280 84102 0 None 3 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 3 5 4.5 COC(=O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
CHEMBL208352 84102 0 None 3 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 3 5 4.5 COC(=O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
56665368 73233 0 None -158 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835854 73233 0 None -158 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852119 73233 0 None -158 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
42625587 19472 0 None -158 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL1187520 19472 0 None -158 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL506518 19472 0 None -158 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
10741134 169521 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 426 9 4 5 3.5 C[C@H](NCCc1cc(Cl)c(N(C)CC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL417137 169521 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 426 9 4 5 3.5 C[C@H](NCCc1cc(Cl)c(N(C)CC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
1960 9632 67 None -1047 19 Rat 5.8 pEC50 = 5.8 Functional
Effective dose for contraction of reserpine-pretreated rat vas deferensEffective dose for contraction of reserpine-pretreated rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 9632 67 None -1047 19 Rat 5.8 pEC50 = 5.8 Functional
Effective dose for contraction of reserpine-pretreated rat vas deferensEffective dose for contraction of reserpine-pretreated rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 9632 67 None -1047 19 Rat 5.8 pEC50 = 5.8 Functional
Effective dose for contraction of reserpine-pretreated rat vas deferensEffective dose for contraction of reserpine-pretreated rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 9632 67 None -1047 19 Rat 5.8 pEC50 = 5.8 Functional
Effective dose for contraction of reserpine-pretreated rat vas deferensEffective dose for contraction of reserpine-pretreated rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 9632 67 None -1047 19 Rat 5.8 pEC50 = 5.8 Functional
Effective dose for contraction of reserpine-pretreated rat vas deferensEffective dose for contraction of reserpine-pretreated rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
9891927 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL446840 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483200 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483201 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
9891927 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL446840 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL483200 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL483201 190976 9 None -10000 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
9803988 207125 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm701324c
CHEMBL59765 207125 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm701324c
24950057 194740 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 471 7 3 4 5.7 O=C(O)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)ccc1Cl 10.1021/jm800222k
CHEMBL497115 194740 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 471 7 3 4 5.7 O=C(O)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)ccc1Cl 10.1021/jm800222k
9803988 207125 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm800222k
CHEMBL59765 207125 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm800222k
9803988 207125 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm8000345
CHEMBL59765 207125 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm8000345
44308088 210376 0 None 316 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL66936 210376 0 None 316 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
46881701 13636 0 None 229 3 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 477 9 3 8 3.0 Cc1sc2ncn(CC(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)c(=O)c2c1C 10.1016/j.bmcl.2010.01.130
CHEMBL1084145 13636 0 None 229 3 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 477 9 3 8 3.0 Cc1sc2ncn(CC(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)c(=O)c2c1C 10.1016/j.bmcl.2010.01.130
14823035 148341 2 None 1 4 Rat 7.8 pEC50 = 7.8 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm00094a025
CHEMBL38486 148341 2 None 1 4 Rat 7.8 pEC50 = 7.8 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm00094a025
9832011 112258 0 None 19 3 Human 7.8 pEC50 = 7.8 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL312074 112258 0 None 19 3 Human 7.8 pEC50 = 7.8 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
76314766 112693 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 405 7 3 6 2.9 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)n1cccn1 10.1021/jm4017224
CHEMBL3128187 112693 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 405 7 3 6 2.9 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)n1cccn1 10.1021/jm4017224
44335497 11594 0 None 50 3 Human 6.8 pEC50 = 6.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 397 9 3 5 2.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00571-x
CHEMBL104180 11594 0 None 50 3 Human 6.8 pEC50 = 6.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 397 9 3 5 2.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00571-x
44517694 201950 0 None -17 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203996 201950 0 None -17 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL550445 201950 0 None -17 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
44392490 72017 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182708 72017 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44286983 148488 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 362 9 3 4 2.5 C[C@H](Cc1ccc(OCC(N)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL38569 148488 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 362 9 3 4 2.5 C[C@H](Cc1ccc(OCC(N)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44287337 157937 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 378 9 4 5 2.5 C[C@H](Cc1ccc(OCC(=O)NO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL39596 157937 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 378 9 4 5 2.5 C[C@H](Cc1ccc(OCC(=O)NO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
10273799 20065 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 422 12 4 6 1.6 COCCNS(=O)(=O)Nc1ccc(CC(C)(C)NC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL1191784 20065 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 422 12 4 6 1.6 COCCNS(=O)(=O)Nc1ccc(CC(C)(C)NC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL542928 20065 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 422 12 4 6 1.6 COCCNS(=O)(=O)Nc1ccc(CC(C)(C)NC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
24823131 104177 0 None 15 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1Cl 10.1021/jm701324c
CHEMBL269823 104177 0 None 15 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1Cl 10.1021/jm701324c
45280075 129141 0 None 91 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3600395 129141 0 None 91 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
3038500 16112 12 None 2 6 Rhesus macaque 7.8 pEC50 = 7.8 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 16112 12 None 2 6 Rhesus macaque 7.8 pEC50 = 7.8 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
44268475 104996 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 671 13 3 8 6.7 CC(C)(C)OC(=O)N(CCc1ccc(NS(=O)(=O)c2ccc(N)cc2)cc1)C[C@H](O)COc1ccc(O[Si](C)(C)C(C)(C)C)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL274312 104996 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 671 13 3 8 6.7 CC(C)(C)OC(=O)N(CCc1ccc(NS(=O)(=O)c2ccc(N)cc2)cc1)C[C@H](O)COc1ccc(O[Si](C)(C)C(C)(C)C)cc1 10.1016/s0960-894x(98)00170-x
44392566 71602 0 None -11 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C=C(C)CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181964 71602 0 None -11 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C=C(C)CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44444175 100797 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 530 11 4 7 3.7 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CCC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL248750 100797 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 530 11 4 7 3.7 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CCC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
10132882 101284 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 355 8 2 6 3.2 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL251599 101284 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 355 8 2 6 3.2 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
9947512 161485 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 369 9 2 6 3.5 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL399785 161485 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 369 9 2 6 3.5 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
45271518 201863 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203999 201863 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL549689 201863 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
10115462 62705 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 459 7 3 6 3.5 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4cccc(Cl)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL162380 62705 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 459 7 3 6 3.5 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4cccc(Cl)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44127681 201995 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 420 11 4 5 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL550746 201995 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 420 11 4 5 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44127054 202065 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL551350 202065 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.ejmech.2009.01.022
46881653 14155 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 380 9 4 6 1.6 Cc1nnc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1086411 14155 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 380 9 4 6 1.6 Cc1nnc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)[nH]1 10.1016/j.bmcl.2010.01.130
46881618 14786 0 None 8 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 458 10 3 6 4.3 O=C(Cc1csc(-c2ccccc2)n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1090746 14786 0 None 8 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 458 10 3 6 4.3 O=C(Cc1csc(-c2ccccc2)n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
46881899 14559 0 None 72 2 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089395 14559 0 None 72 2 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.01.130
44335603 114207 0 None 446 3 Human 7.8 pEC50 = 7.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 538 16 4 6 5.0 CCCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL318165 114207 0 None 446 3 Human 7.8 pEC50 = 7.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 538 16 4 6 5.0 CCCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44335562 115318 0 None 112 3 Human 7.8 pEC50 = 7.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 558 14 4 6 4.7 O=C(CCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL320138 115318 0 None 112 3 Human 7.8 pEC50 = 7.8 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 558 14 4 6 4.7 O=C(CCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
10118962 20412 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 523 11 3 6 3.2 CC(C)(Cc1ccc(NS(=O)(=O)N2CCN(Cc3ccccc3)CC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL1194452 20412 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 523 11 3 6 3.2 CC(C)(Cc1ccc(NS(=O)(=O)N2CCN(Cc3ccccc3)CC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL552668 20412 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 523 11 3 6 3.2 CC(C)(Cc1ccc(NS(=O)(=O)N2CCN(Cc3ccccc3)CC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
24823470 104216 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 10 3 4 4.3 O=C(O)COc1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL270025 104216 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 10 3 4 4.3 O=C(O)COc1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
24885648 23908 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 460 8 2 7 4.4 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1255596 23908 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 460 8 2 7 4.4 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
42639806 19290 0 None 40 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 468 10 3 6 2.9 COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186584 19290 0 None 40 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 468 10 3 6 2.9 COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL470858 19290 0 None 40 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 468 10 3 6 2.9 COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44461489 212131 0 None 363 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 13 3 6 4.3 O=C1N(CCCC(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL79675 212131 0 None 363 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 13 3 6 4.3 O=C1N(CCCC(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
10099459 212475 1 None 128 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
10099459 212475 1 None 128 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL82296 212475 1 None 128 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL82296 212475 1 None 128 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
44396681 74148 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 10 4 6 2.2 CCS(=O)(=O)Nc1cccc([C@@H](O)CNCCc2c[nH]c3c(S(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.09.054
CHEMBL188663 74148 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 10 4 6 2.2 CCS(=O)(=O)Nc1cccc([C@@H](O)CNCCc2c[nH]c3c(S(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.09.054
44307065 210111 0 None 50 3 Human 7.8 pEC50 = 7.8 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 445 11 3 6 2.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(F)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64932 210111 0 None 50 3 Human 7.8 pEC50 = 7.8 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 445 11 3 6 2.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(F)cc1 10.1016/s0960-894x(98)00381-3
44307166 109498 0 None 5 3 Human 7.8 pEC50 = 7.8 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 570 11 3 5 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(F)cc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL304878 109498 0 None 5 3 Human 7.8 pEC50 = 7.8 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 570 11 3 5 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(F)cc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
44298781 107470 0 None 54 3 Human 7.8 pEC50 = 7.8 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 10 1 3 5.3 CCCCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL292407 107470 0 None 54 3 Human 7.8 pEC50 = 7.8 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 10 1 3 5.3 CCCCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
15483879 106559 0 None 223 3 Human 7.8 pEC50 = 7.8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285240 106559 0 None 223 3 Human 7.8 pEC50 = 7.8 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
12049918 108987 0 None 72 3 Human 7.8 pEC50 = 7.8 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 624 12 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL302893 108987 0 None 72 3 Human 7.8 pEC50 = 7.8 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 624 12 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
10274448 20086 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 432 10 3 5 2.9 CN(C1CCCCC1)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL1191988 20086 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 432 10 3 5 2.9 CN(C1CCCCC1)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL543162 20086 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 432 10 3 5 2.9 CN(C1CCCCC1)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
24812043 102843 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@H](Oc1ccc(CCNC[C@@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL260018 102843 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@H](Oc1ccc(CCNC[C@@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
46881900 14560 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1089396 14560 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2010.01.130
76322045 112690 0 None 13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 527 7 3 5 6.0 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
CHEMBL3128184 112690 0 None 13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 527 7 3 5 6.0 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
46881901 14617 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089734 14617 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
44331766 11430 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 449 9 3 4 4.3 O[C@@H](CNCC1CCN(CCC(F)(F)F)CC1)COc1cccc2[nH]c3ccccc3c12 10.1016/s0960-894x(02)00607-8
CHEMBL103137 11430 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 449 9 3 4 4.3 O[C@@H](CNCC1CCN(CCC(F)(F)F)CC1)COc1cccc2[nH]c3ccccc3c12 10.1016/s0960-894x(02)00607-8
12043157 123528 0 None 34 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 589 14 3 8 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
CHEMBL33755 123528 0 None 34 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 589 14 3 8 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
46881699 12365 0 None 177 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 9 3 7 2.3 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1077238 12365 0 None 177 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 9 3 7 2.3 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
46881700 13635 0 None 158 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 9 3 7 2.3 O=C(Cn1c(=O)ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084144 13635 0 None 158 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 9 3 7 2.3 O=C(Cn1c(=O)ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
46881531 13761 0 None 501 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 4 5 3.0 O=C(Cc1n[nH]c2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084667 13761 0 None 501 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 4 5 3.0 O=C(Cc1n[nH]c2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
12017015 129872 0 None 131 3 Human 7.7 pEC50 = 7.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 546 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL36101 129872 0 None 131 3 Human 7.7 pEC50 = 7.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 546 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
12017013 143059 0 None 338 3 Human 7.7 pEC50 = 7.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 588 13 3 8 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL37335 143059 0 None 338 3 Human 7.7 pEC50 = 7.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 588 13 3 8 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
10841171 123802 0 None 131 3 Human 7.7 pEC50 = 7.7 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3F)cs2)cc1 10.1021/jm000286i
CHEMBL338976 123802 0 None 131 3 Human 7.7 pEC50 = 7.7 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3F)cs2)cc1 10.1021/jm000286i
11026016 53474 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 411 10 4 5 2.5 C[C@H](CNc1ccc(CNS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL153916 53474 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 411 10 4 5 2.5 C[C@H](CNc1ccc(CNS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
10902809 54851 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 304 7 3 3 3.5 C[C@H](CNc1ccccc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL155072 54851 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 304 7 3 3 3.5 C[C@H](CNc1ccccc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11005613 126577 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348269 126577 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
44281425 107083 0 None 15 3 Human 6.7 pEC50 = 6.7 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 612 13 4 9 4.3 CC(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL289250 107083 0 None 15 3 Human 6.7 pEC50 = 6.7 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 612 13 4 9 4.3 CC(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
31729 212563 10 None -7 7 Rat 6.7 pEC50 = 6.7 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 287 6 4 4 2.4 CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL83063 212563 10 None -7 7 Rat 6.7 pEC50 = 6.7 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 287 6 4 4 2.4 CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1 10.1021/jm000455z
44392212 175148 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204383 175148 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL434524 175148 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
56675509 71270 0 None -79 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814270 71270 0 None -79 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
9849126 19211 0 None -5011 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL1185969 19211 0 None -5011 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL443435 19211 0 None -5011 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
42625743 19373 0 None 12 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186943 19373 0 None 12 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483407 19373 0 None 12 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
11605652 19327 0 None -1995 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186715 19327 0 None -1995 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475236 19327 0 None -1995 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
3038500 16112 12 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 16112 12 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
24822645 102268 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(Cl)c1 10.1021/jm701324c
CHEMBL257297 102268 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(Cl)c1 10.1021/jm701324c
24822974 104588 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL271945 104588 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
24950718 182777 0 None 398 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(C(=O)O)ccc1-c1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(Cl)cc1)CC2 10.1021/jm800222k
CHEMBL458927 182777 0 None 398 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(C(=O)O)ccc1-c1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(Cl)cc1)CC2 10.1021/jm800222k
24937137 24530 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258707 24530 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
1499 8872 47 None -190 38 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
3779 8872 47 None -190 38 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
536 8872 47 None -190 38 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
CHEMBL434 8872 47 None -190 38 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
DB01064 8872 47 None -190 38 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
24822974 104588 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL271945 104588 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24822974 104588 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL271945 104588 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
76322043 112684 0 None -1 4 Rhesus macaque 8.7 pEC50 = 8.7 Functional
Agonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
CHEMBL3128178 112684 0 None -1 4 Rhesus macaque 8.7 pEC50 = 8.7 Functional
Agonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
44396509 74073 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 513 11 4 6 5.1 CC(C)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL188315 74073 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 513 11 4 6 5.1 CC(C)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
44396615 74082 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 513 10 4 6 3.2 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccccc4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188368 74082 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 513 10 4 6 3.2 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccccc4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
142109146 136599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 607 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)c5c4CCC(=O)N5)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44385888 136599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 607 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)c5c4CCC(=O)N5)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
69923118 136599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 607 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)c5c4CCC(=O)N5)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
88054366 136599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 607 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)c5c4CCC(=O)N5)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
CHEMBL367561 136599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 607 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)c5c4CCC(=O)N5)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44402691 148089 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 619 12 3 6 7.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL383379 148089 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 619 12 3 6 7.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301842 205650 0 None 3162 3 Human 8.7 pEC50 = 8.7 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 606 11 3 7 6.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL58407 205650 0 None 3162 3 Human 8.7 pEC50 = 8.7 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 606 11 3 7 6.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44281530 106596 0 None 363 3 Human 8.7 pEC50 = 8.7 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 609 12 3 8 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cc(F)c(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285499 106596 0 None 363 3 Human 8.7 pEC50 = 8.7 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 609 12 3 8 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cc(F)c(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44280904 106737 0 None 1047 3 Human 8.7 pEC50 = 8.7 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 632 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(-c4ccccn4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286438 106737 0 None 1047 3 Human 8.7 pEC50 = 8.7 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 632 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(-c4ccccn4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
145983829 172528 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 557 15 6 5 5.9 CCCCCC(=O)Nc1ccccc1NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4246625 172528 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 557 15 6 5 5.9 CCCCCC(=O)Nc1ccccc1NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
9804536 172476 0 None 7 3 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 465 11 4 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4245391 172476 0 None 7 3 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 465 11 4 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
127037832 144830 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
24895192 196643 0 None 151 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 437 10 3 4 4.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(F)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL516804 196643 0 None 151 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 437 10 3 4 4.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(F)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44268570 104971 0 None 346 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 598 17 5 7 4.8 CCCCCCN(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL274144 104971 0 None 346 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 598 17 5 7 4.8 CCCCCCN(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44392228 71636 0 None 7 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 441 11 5 5 3.1 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)NC1CCCCC1 10.1016/j.bmcl.2004.11.001
CHEMBL182127 71636 0 None 7 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 441 11 5 5 3.1 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)NC1CCCCC1 10.1016/j.bmcl.2004.11.001
145985509 172427 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 472 12 5 4 4.1 O=C(NCCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4244123 172427 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 472 12 5 4 4.1 O=C(NCCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
567 7512 16 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
9841972 7512 16 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
CHEMBL284782 7512 16 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
567 7512 16 None 2 7 Rat 8.7 pEC50 = 8.7 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
9841972 7512 16 None 2 7 Rat 8.7 pEC50 = 8.7 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
CHEMBL284782 7512 16 None 2 7 Rat 8.7 pEC50 = 8.7 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
10002049 104217 0 None -3 2 Dog 8.7 pEC50 = 8.7 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL270026 104217 0 None -3 2 Dog 8.7 pEC50 = 8.7 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 417 10 3 3 5.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44472612 144696 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1cccnc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3763594 144696 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1cccnc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
24823627 164898 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 467 10 3 5 4.1 CC(C)S(=O)(=O)c1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL408693 164898 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 467 10 3 5 4.1 CC(C)S(=O)(=O)c1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
24937013 24221 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 9 3 8 4.6 CCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257676 24221 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 9 3 8 4.6 CCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
15523859 212712 0 None 173 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
15523859 212712 0 None 173 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL84190 212712 0 None 173 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL84190 212712 0 None 173 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
567 7512 16 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
9841972 7512 16 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
CHEMBL284782 7512 16 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
44268478 169593 0 None 47 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 561 13 5 7 4.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00170-x
CHEMBL417250 169593 0 None 47 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 561 13 5 7 4.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00170-x
12017017 134259 0 None 1513 3 Human 8.6 pEC50 = 8.6 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 606 13 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL36609 134259 0 None 1513 3 Human 8.6 pEC50 = 8.6 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 606 13 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
9849699 80039 16 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012520 80039 16 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012521 80039 16 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012522 80039 16 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at human adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
24950409 200226 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 427 6 3 4 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)s1 10.1021/jm800222k
CHEMBL526472 200226 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 427 6 3 4 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)s1 10.1021/jm800222k
24895667 183630 0 None 208 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL461282 183630 0 None 208 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24894319 196638 0 None 213 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 11 3 5 4.5 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL516785 196638 0 None 213 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 11 3 5 4.5 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44268572 32437 0 None 416 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 572 16 6 8 2.9 COCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13521 32437 0 None 416 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 572 16 6 8 2.9 COCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44396654 129971 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 531 10 4 6 3.4 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(F)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL361300 129971 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 531 10 4 6 3.4 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(F)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44402733 140883 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 625 12 3 6 7.4 CC(C)(C)c1ccc(-c2csc(Cc3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5ccccc5)cc4)cc3)n2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL371641 140883 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 625 12 3 6 7.4 CC(C)(C)c1ccc(-c2csc(Cc3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5ccccc5)cc4)cc3)n2)cc1 10.1016/j.bmcl.2005.03.119
44298497 201478 0 None 218 3 Human 8.6 pEC50 = 8.6 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 464 11 1 5 5.9 CCCCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL53359 201478 0 None 218 3 Human 8.6 pEC50 = 8.6 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 464 11 1 5 5.9 CCCCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
44301819 107839 0 None 660 3 Human 8.6 pEC50 = 8.6 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 612 11 3 7 6.8 CC(C)(C)c1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL294753 107839 0 None 660 3 Human 8.6 pEC50 = 8.6 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 612 11 3 7 6.8 CC(C)(C)c1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
145983629 172674 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 462 10 5 4 4.5 O=C(Nc1ccc(F)cc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4249769 172674 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 462 10 5 4 4.5 O=C(Nc1ccc(F)cc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
52949488 24318 0 None 3 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258023 24318 0 None 3 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
127037832 144830 0 None -2 4 Rhesus macaque 8.6 pEC50 = 8.6 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None -2 4 Rhesus macaque 8.6 pEC50 = 8.6 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
44377315 64149 0 None 398 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 605 14 3 6 5.4 O=C1N(CCCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL165177 64149 0 None 398 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 605 14 3 6 5.4 O=C1N(CCCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44392215 72376 0 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183307 72376 0 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.11.001
42640122 202954 0 None -2 2 Dog 8.6 pEC50 = 8.6 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL492401 202954 0 None -2 2 Dog 8.6 pEC50 = 8.6 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL561335 202954 0 None -2 2 Dog 8.6 pEC50 = 8.6 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
56678973 73353 0 None -2 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835855 73353 0 None -2 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852541 73353 0 None -2 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
44268320 25198 0 None 58 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 456 11 4 6 3.1 Cc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12718 25198 0 None 58 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 456 11 4 6 3.1 Cc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
127026491 144722 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 433 7 3 7 2.2 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3763998 144722 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 433 7 3 7 2.2 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
24895671 185673 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 4 5 4.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL469884 185673 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 4 5 4.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44377753 126708 0 None 5011 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 605 12 3 8 4.0 O=c1n(Cc2ccc(F)c(F)c2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL349505 126708 0 None 5011 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 605 12 3 8 4.0 O=c1n(Cc2ccc(F)c(F)c2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44268479 27661 0 None 81 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 543 13 5 8 3.7 CC(C)OC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13106 27661 0 None 81 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 543 13 5 8 3.7 CC(C)OC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
145983617 172646 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 517 11 6 6 4.6 COC(=O)Nc1ccccc1NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4249199 172646 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 517 11 6 6 4.6 COC(=O)Nc1ccccc1NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
24812044 102715 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@H](Oc1ccc(CCNC[C@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL259361 102715 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@H](Oc1ccc(CCNC[C@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
44444171 101278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 546 13 4 7 4.3 CCC1(CC)C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
CHEMBL251579 101278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 546 13 4 7 4.3 CCC1(CC)C(=O)Nc2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2007.09.011
127037832 144830 0 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
44402694 76300 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc4ncccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL193410 76300 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc4ncccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301806 107496 0 None 2238 3 Human 8.6 pEC50 = 8.6 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ncccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL292598 107496 0 None 2238 3 Human 8.6 pEC50 = 8.6 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ncccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
11165102 100749 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 386 8 3 3 4.9 CC(Cc1c[nH]c2c(OC(C)C)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24851 100749 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 386 8 3 3 4.9 CC(Cc1c[nH]c2c(OC(C)C)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
24949418 194893 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
CHEMBL498302 194893 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
52946537 24495 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258599 24495 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
42639311 19296 0 None 56 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186600 19296 0 None 56 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL472089 19296 0 None 56 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44268604 43398 0 None 70 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 598 18 6 7 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL144870 43398 0 None 70 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 598 18 6 7 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44396574 74053 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 597 10 4 7 4.1 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccc(Br)s4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188178 74053 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 597 10 4 7 4.1 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccc(Br)s4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
145985368 172722 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 450 10 5 4 4.2 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)NC1CCCCC1 10.1016/j.ejmech.2018.03.032
CHEMBL4251063 172722 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 450 10 5 4 4.2 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)NC1CCCCC1 10.1016/j.ejmech.2018.03.032
24822974 104588 0 None -1 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL271945 104588 0 None -1 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
24822974 104588 0 None -1 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL271945 104588 0 None -1 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639810 19283 0 None -4 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 530 11 3 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
CHEMBL1186551 19283 0 None -4 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 530 11 3 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
CHEMBL469396 19283 0 None -4 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 530 11 3 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
24822974 104588 0 None -1 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL271945 104588 0 None -1 2 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 419 10 3 4 4.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
24936627 24458 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 444 8 4 9 2.2 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258485 24458 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 444 8 4 9 2.2 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
44392542 72636 0 None 6 3 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL183552 72636 0 None 6 3 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2004.12.033
145984563 172573 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 462 10 5 4 4.5 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)Nc1cccc(F)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4247910 172573 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 462 10 5 4 4.5 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)Nc1cccc(F)c1 10.1016/j.ejmech.2018.03.032
9858463 100909 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2cocn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL249336 100909 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2cocn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
24950240 183789 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 404 7 3 5 3.8 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccnc2)CC3)c1 10.1021/jm800222k
CHEMBL462780 183789 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 404 7 3 5 3.8 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccnc2)CC3)c1 10.1021/jm800222k
24936488 24421 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258373 24421 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
44377687 64218 0 None 50 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 579 16 3 6 5.0 CCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL165513 64218 0 None 50 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 579 16 3 6 5.0 CCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
9915235 211176 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 539 10 3 7 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1OC 10.1016/s0960-894x(03)00387-1
CHEMBL71948 211176 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 539 10 3 7 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1OC 10.1016/s0960-894x(03)00387-1
44396784 74175 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 513 12 4 6 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)CCCCl)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188815 74175 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 513 12 4 6 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)CCCCl)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
9827999 137682 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 519 9 5 10 0.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(Cn4oc(=O)[nH]c4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL368584 137682 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 519 9 5 10 0.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(Cn4oc(=O)[nH]c4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
10145446 10955 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 602 14 5 8 3.6 O=C(NCCCc1cccs1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100124 10955 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 602 14 5 8 3.6 O=C(NCCCc1cccs1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
10575455 106754 1 None 13 3 Human 7.7 pEC50 = 7.7 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 448 8 5 7 1.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(N)=O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL286574 106754 1 None 13 3 Human 7.7 pEC50 = 7.7 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 448 8 5 7 1.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(N)=O)cc3)CC2)ccc1O 10.1021/jm000544b
44268305 105073 0 None -19 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL274782 105073 0 None -19 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
10201549 101285 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 409 8 2 6 3.9 O[C@@H](CNCCOc1ccc(-c2csc(C(F)(F)F)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL251600 101285 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 409 8 2 6 3.9 O[C@@H](CNCCOc1ccc(-c2csc(C(F)(F)F)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
9858464 162297 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2cnco2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL404209 162297 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2cnco2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
44574757 185264 0 None 12 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 511 14 3 6 4.4 O=C(Cc1cccc(OCc2ccccc2)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466467 185264 0 None 12 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 511 14 3 6 4.4 O=C(Cc1cccc(OCc2ccccc2)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
44517696 202550 0 None -17 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204007 202550 0 None -17 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL557705 202550 0 None -17 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
10168241 12050 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 633 19 6 8 4.3 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)c(NS(C)(=O)=O)c3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL106512 12050 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 633 19 6 8 4.3 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)c(NS(C)(=O)=O)c3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44268262 26207 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@H](C)NC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12949 26207 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@H](C)NC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
49861320 61740 0 None -20 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204003 61740 0 None -20 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1615579 61740 0 None -20 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
2687 7676 16 None -162 2 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1016/S0960-894X(96)00603-8
532 7676 16 None -162 2 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1016/S0960-894X(96)00603-8
5387 7676 16 None -162 2 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1016/S0960-894X(96)00603-8
CHEMBL420746 7676 16 None -162 2 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1016/S0960-894X(96)00603-8
44311371 210910 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 317 9 3 5 2.0 COc1ccc(CCNC[C@@H](O)COc2cccc(O)c2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL70403 210910 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 317 9 3 5 2.0 COc1ccc(CCNC[C@@H](O)COc2cccc(O)c2)cc1 10.1016/S0960-894X(96)00603-8
53326196 65430 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684580 65430 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
567 7512 16 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
9841972 7512 16 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
CHEMBL284782 7512 16 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
44580041 200087 0 None 9 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(O)c1cc(NC(=O)c2ccccc2)cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
CHEMBL524145 200087 0 None 9 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(O)c1cc(NC(=O)c2ccccc2)cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
52949489 24319 0 None 12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258024 24319 0 None 12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
10135864 129296 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601200 129296 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44377517 64006 0 None 239 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 551 14 3 6 4.2 CCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL165015 64006 0 None 239 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 551 14 3 6 4.2 CCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
46881936 13939 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 427 9 4 5 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1ncc[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1085442 13939 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 427 9 4 5 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1ncc[nH]1 10.1016/j.bmcl.2010.01.130
46881576 14616 0 None 28 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 416 9 3 6 3.3 O=C(Cc1nc2ccccc2o1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089725 14616 0 None 28 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 416 9 3 6 3.3 O=C(Cc1nc2ccccc2o1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44396678 133317 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 441 9 4 5 3.9 O=S(=O)(Nc1cccc([C@@H](O)CNCCc2c[nH]c3ccccc23)c1)c1cccs1 10.1016/j.bmcl.2004.09.054
CHEMBL365215 133317 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 441 9 4 5 3.9 O=S(=O)(Nc1cccc([C@@H](O)CNCCc2c[nH]c3ccccc23)c1)c1cccs1 10.1016/j.bmcl.2004.09.054
12017018 149116 0 None 95 3 Human 6.7 pEC50 = 6.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 638 13 3 8 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38861 149116 0 None 95 3 Human 6.7 pEC50 = 6.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 638 13 3 8 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
46881798 15349 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 365 9 3 6 1.8 O=C(Cn1cccn1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1094715 15349 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 365 9 3 6 1.8 O=C(Cn1cccn1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
11222097 174090 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1ccc2c(CC(C)NCC(O)c3cccc(Cl)c3)c[nH]c2c1 10.1016/s0960-894x(03)00073-8
CHEMBL429396 174090 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1ccc2c(CC(C)NCC(O)c3cccc(Cl)c3)c[nH]c2c1 10.1016/s0960-894x(03)00073-8
70792359 112694 0 None -5 4 Dog 7.7 pEC50 = 7.7 Functional
Agonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
CHEMBL3128188 112694 0 None -5 4 Dog 7.7 pEC50 = 7.7 Functional
Agonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
24949260 194657 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 9 3 5 4.8 O=C(O)COc1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL496467 194657 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 9 3 5 4.8 O=C(O)COc1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
46881615 15181 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 381 9 4 8 0.8 Nc1ncn(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
CHEMBL1093387 15181 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 381 9 4 8 0.8 Nc1ncn(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
44392238 72309 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 524 11 6 5 4.9 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2cccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183080 72309 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 524 11 6 5 4.9 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2cccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2004.11.001
44402730 148018 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 570 12 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccccn3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL382962 148018 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 570 12 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccccn3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44307063 210113 0 None 10 3 Human 7.7 pEC50 = 7.7 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 505 11 3 6 3.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64935 210113 0 None 10 3 Human 7.7 pEC50 = 7.7 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 505 11 3 6 3.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00381-3
44307333 210453 0 None 28 3 Human 7.7 pEC50 = 7.7 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 472 12 4 8 2.0 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL67416 210453 0 None 28 3 Human 7.7 pEC50 = 7.7 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 472 12 4 8 2.0 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
12017006 107173 0 None 64 3 Human 7.7 pEC50 = 7.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 608 11 3 7 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL290053 107173 0 None 64 3 Human 7.7 pEC50 = 7.7 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 608 11 3 7 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
44301804 174960 0 None 181 3 Human 7.7 pEC50 = 7.7 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccn3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL433248 174960 0 None 181 3 Human 7.7 pEC50 = 7.7 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccn3)cs2)cc1 10.1016/s0960-894x(00)00390-5
12049917 209805 0 None 114 3 Human 7.7 pEC50 = 7.7 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 588 12 3 9 4.1 COc1ccc(-c2cnn(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1F 10.1016/s0960-894x(00)00422-4
CHEMBL63357 209805 0 None 114 3 Human 7.7 pEC50 = 7.7 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 588 12 3 9 4.1 COc1ccc(-c2cnn(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1F 10.1016/s0960-894x(00)00422-4
10690668 127377 0 None 478 2 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 372 9 5 5 2.9 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL35459 127377 0 None 478 2 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 372 9 5 5 2.9 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
11270071 105766 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279931 105766 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
10297331 101141 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 445 12 2 7 4.2 O[C@@H](CNCCOc1ccc(-c2coc(COCc3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250760 101141 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 445 12 2 7 4.2 O[C@@H](CNCCOc1ccc(-c2coc(COCc3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
44377483 64262 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 463 8 4 7 1.8 CN(c1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)O)cc3)CC2)ccc1O)S(C)(=O)=O 10.1016/s0960-894x(01)00063-4
CHEMBL165892 64262 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 463 8 4 7 1.8 CN(c1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)O)cc3)CC2)ccc1O)S(C)(=O)=O 10.1016/s0960-894x(01)00063-4
9803765 106423 0 None 223 2 Human 6.7 pEC50 = 6.7 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 449 8 5 7 1.8 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284311 106423 0 None 223 2 Human 6.7 pEC50 = 6.7 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 449 8 5 7 1.8 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
44311119 171304 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 357 9 4 6 1.8 COc1ccc(CCNC[C@@H](O)COc2cccc3[nH]c(O)nc23)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL421489 171304 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 357 9 4 6 1.8 COc1ccc(CCNC[C@@H](O)COc2cccc3[nH]c(O)nc23)cc1 10.1016/S0960-894X(96)00603-8
46881529 14034 0 None 13 2 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 375 9 3 4 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1085898 14034 0 None 13 2 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 375 9 3 4 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44444359 101282 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 353 8 2 5 3.6 CCc1nc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL251592 101282 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 353 8 2 5 3.6 CCc1nc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
10162876 19691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 480 10 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)N1CCC(c2ccccc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL1189086 19691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 480 10 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)N1CCC(c2ccccc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL538024 19691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 480 10 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)N1CCC(c2ccccc2)CC1 10.1016/s0960-894x(04)00462-7
10007337 123478 0 None 131 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 535 14 3 8 4.5 CCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33725 123478 0 None 131 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 535 14 3 8 4.5 CCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44307186 210547 0 None 4 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 455 12 3 6 3.0 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL68021 210547 0 None 4 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 455 12 3 6 3.0 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
10209574 12211 0 None 22 2 Human 7.6 pEC50 = 7.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1cc(F)ccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107382 12211 0 None 22 2 Human 7.6 pEC50 = 7.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1cc(F)ccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
11791723 117342 0 None 26 2 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 344 9 5 5 2.1 C[C@H](NCCc1ccc(NCC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32532 117342 0 None 26 2 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 344 9 5 5 2.1 C[C@H](NCCc1ccc(NCC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44444367 101055 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 465 9 3 6 4.0 Cc1nc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)c(NS(C)(=O)=O)c3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL250385 101055 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 465 9 3 6 4.0 Cc1nc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)c(NS(C)(=O)=O)c3)cc2)cs1 10.1016/j.bmcl.2007.06.072
45271517 201830 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203998 201830 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549487 201830 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45272430 202223 0 None -36 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204001 202223 0 None -36 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552374 202223 0 None -36 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
44385592 179547 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 516 9 6 9 0.4 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(CC4N=C(N)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL451185 179547 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 516 9 6 9 0.4 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(CC4N=C(N)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
44285225 160355 0 None 4 3 Human 6.6 pEC50 = 6.6 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 562 13 3 7 5.8 CC(C)(C)CCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL39804 160355 0 None 4 3 Human 6.6 pEC50 = 6.6 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 562 13 3 7 5.8 CC(C)(C)CCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
46889771 13766 0 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084706 13766 0 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
24812045 103023 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@@H](Oc1ccc(CCNC[C@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL260996 103023 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 C[C@@H](Oc1ccc(CCNC[C@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
10296491 19982 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 432 9 3 5 2.6 C[C@H]1C[C@@H](C)CN(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)C1 10.1016/s0960-894x(04)00462-7
CHEMBL1191144 19982 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 432 9 3 5 2.6 C[C@H]1C[C@@H](C)CN(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)C1 10.1016/s0960-894x(04)00462-7
CHEMBL542200 19982 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 432 9 3 5 2.6 C[C@H]1C[C@@H](C)CN(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)C1 10.1016/s0960-894x(04)00462-7
50995330 143781 0 None 218 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 422 7 4 6 3.1 Nc1nc(CNC(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2015.11.030
CHEMBL3746068 143781 0 None 218 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 422 7 4 6 3.1 Nc1nc(CNC(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2015.11.030
24949885 200160 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 9 3 5 4.8 O=C(O)COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
CHEMBL525358 200160 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 9 3 5 4.8 O=C(O)COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
52948728 24219 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257674 24219 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
44377523 63005 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 509 9 3 8 1.0 O=C1N=c2cccc(OC[C@@H](O)CNC3CCN(c4ccc(CC5SC(=O)NC5=O)cc4)CC3)c2=N1 10.1016/s0960-894x(01)00063-4
CHEMBL162711 63005 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 509 9 3 8 1.0 O=C1N=c2cccc(OC[C@@H](O)CNC3CCN(c4ccc(CC5SC(=O)NC5=O)cc4)CC3)c2=N1 10.1016/s0960-894x(01)00063-4
46881981 12512 0 None 288 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCn1cccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078395 12512 0 None 288 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCn1cccc1 10.1016/j.bmcl.2010.01.130
46881575 14556 0 None 316 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 416 9 3 7 2.3 O=C(Cn1nc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089387 14556 0 None 316 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 416 9 3 7 2.3 O=C(Cn1nc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44306956 210126 0 None 12 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 495 11 3 6 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00381-3
CHEMBL65042 210126 0 None 12 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 495 11 3 6 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00381-3
12049915 109616 0 None 389 3 Human 7.6 pEC50 = 7.6 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL305558 109616 0 None 389 3 Human 7.6 pEC50 = 7.6 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
12049921 210356 0 None 208 3 Human 7.6 pEC50 = 7.6 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cccc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL66789 210356 0 None 208 3 Human 7.6 pEC50 = 7.6 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cccc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
44444153 101210 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 490 11 4 7 2.8 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1CC(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL251167 101210 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 490 11 4 7 2.8 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1CC(=O)N2 10.1016/j.bmcl.2007.09.011
44419332 148538 0 None -3 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 505 11 4 8 2.5 Cn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
CHEMBL386016 148538 0 None -3 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 505 11 4 8 2.5 Cn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
11270069 102476 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25823 102476 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
44126933 202944 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561291 202944 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
4421983 14051 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 484 9 1 5 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086005 14051 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 484 9 1 5 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
46881799 15397 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.1 Cc1ccn(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
CHEMBL1095042 15397 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.1 Cc1ccn(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
52948612 24102 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 9 3 8 4.1 O=C(O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257323 24102 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 504 9 3 8 4.1 O=C(O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
127037832 144830 0 None -147 4 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None -147 4 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
10138551 20670 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 446 10 4 5 3.3 CC(C)(Cc1ccc(NS(=O)(=O)NC2CCCCC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL1196238 20670 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 446 10 4 5 3.3 CC(C)(Cc1ccc(NS(=O)(=O)NC2CCCCC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL556202 20670 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 446 10 4 5 3.3 CC(C)(Cc1ccc(NS(=O)(=O)NC2CCCCC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
44268266 24780 0 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 317 8 4 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12633 24780 0 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 317 8 4 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
44268277 29080 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 408 11 4 6 2.1 CC(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13238 29080 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 408 11 4 6 2.1 CC(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
3038500 16112 12 None -9 6 Dog 7.6 pEC50 = 7.6 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 16112 12 None -9 6 Dog 7.6 pEC50 = 7.6 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
24949720 196301 0 None -66 3 Dog 7.6 pEC50 = 7.6 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1 10.1021/jm800222k
CHEMBL514102 196301 0 None -66 3 Dog 7.6 pEC50 = 7.6 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1 10.1021/jm800222k
44377755 126732 0 None 398 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 589 13 3 8 4.0 O=c1n(CCCC(F)(F)F)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL349689 126732 0 None 398 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 589 13 3 8 4.0 O=c1n(CCCC(F)(F)F)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44396616 74286 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 455 9 4 5 4.2 Cc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL189518 74286 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 455 9 4 5 4.2 Cc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
567 7512 16 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0101500
9841972 7512 16 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0101500
CHEMBL284782 7512 16 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0101500
11003341 53071 0 None 10 3 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL153558 53071 0 None 10 3 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
567 7512 16 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0509445
9841972 7512 16 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0509445
CHEMBL284782 7512 16 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0509445
1239 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3465 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
CHEMBL1256786 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
DB00983 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
56678849 73400 0 None -31 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814275 73400 0 None -31 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1852744 73400 0 None -31 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
11003341 53071 0 None 10 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL153558 53071 0 None 10 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
1239 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
11592062 119234 0 None -158 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
CHEMBL3298325 119234 0 None -158 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
3083544 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1200811 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1363 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1951071 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL605993 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
56675663 73363 0 None -25 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835861 73363 0 None -25 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852575 73363 0 None -25 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
1239 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3410 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3465 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
CHEMBL1256786 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
DB00983 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3083544 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL1200811 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL1363 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL1951071 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL605993 33582 51 None -16 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
1239 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 8458 55 None -79 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
146015362 7734 10 None -15 5 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
3462 7734 10 None -15 5 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
5486546 7734 10 None -15 5 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
CHEMBL1204876 7734 10 None -15 5 Rat 7.6 pEC50 = 7.6 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
44219641 185218 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 3 6 4.1 CC(Cc1ccc(NC(=O)Cc2nccn2Cc2ccccc2)cc1)NC[C@H](O)COc1ccccc1 10.1016/j.bmc.2009.03.044
CHEMBL466088 185218 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 3 6 4.1 CC(Cc1ccc(NC(=O)Cc2nccn2Cc2ccccc2)cc1)NC[C@H](O)COc1ccccc1 10.1016/j.bmc.2009.03.044
10232096 114442 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 586 12 5 6 5.1 O=C(NCc1ccc(Cl)cc1Cl)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL319041 114442 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 586 12 5 6 5.1 O=C(NCc1ccc(Cl)cc1Cl)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
42625741 19371 0 None -316 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186940 19371 0 None -316 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483202 19371 0 None -316 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625588 187205 0 None -1584 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475237 187205 0 None -1584 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
24937269 24419 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258371 24419 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
10291064 101255 0 None 1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat adrenergic beta-3 receptor assessed as cAMP productionAgonist activity at rat adrenergic beta-3 receptor assessed as cAMP production
ChEMBL 341 8 2 6 2.9 O[C@@H](CNCCOc1ccc(-c2cscn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL251392 101255 0 None 1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat adrenergic beta-3 receptor assessed as cAMP productionAgonist activity at rat adrenergic beta-3 receptor assessed as cAMP production
ChEMBL 341 8 2 6 2.9 O[C@@H](CNCCOc1ccc(-c2cscn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
44402690 77881 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 589 14 3 6 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(CCC3CCCC3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL195400 77881 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 589 14 3 6 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(CCC3CCCC3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44307340 109372 0 None 4 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 470 12 4 7 2.6 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL304090 109372 0 None 4 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 470 12 4 7 2.6 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44306985 210498 0 None 38 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 460 11 4 7 2.2 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(F)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67672 210498 0 None 38 3 Human 7.6 pEC50 = 7.6 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 460 11 4 7 2.2 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(F)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
10166311 11134 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 555 11 5 8 2.9 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)Nc1ccccn1 10.1016/s0960-894x(02)00607-8
CHEMBL101132 11134 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 555 11 5 8 2.9 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)Nc1ccccn1 10.1016/s0960-894x(02)00607-8
44285529 157697 0 None 7 3 Human 7.6 pEC50 = 7.6 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 534 14 3 7 5.1 CCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL39577 157697 0 None 7 3 Human 7.6 pEC50 = 7.6 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 534 14 3 7 5.1 CCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
10602703 127096 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 548 11 6 8 1.9 CC(C)[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
CHEMBL35282 127096 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 548 11 6 8 1.9 CC(C)[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
44301831 107740 0 None 114 3 Human 7.6 pEC50 = 7.6 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 590 14 3 7 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCCC3CCCC3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL294172 107740 0 None 114 3 Human 7.6 pEC50 = 7.6 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 590 14 3 7 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCCC3CCCC3)cs2)cc1 10.1016/s0960-894x(00)00390-5
69655138 85943 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 520 11 6 8 1.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL2113344 85943 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 520 11 6 8 1.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
46881796 12370 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 401 8 3 6 2.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc2ccnn12 10.1016/j.bmcl.2010.01.130
CHEMBL1077273 12370 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 401 8 3 6 2.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc2ccnn12 10.1016/j.bmcl.2010.01.130
52941476 24457 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 488 9 2 7 4.9 CCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258484 24457 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 488 9 2 7 4.9 CCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
44286964 170175 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 399 9 4 4 3.1 C[C@H](Cc1ccc(OCP(=O)(O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL41948 170175 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 399 9 4 4 3.1 C[C@H](Cc1ccc(OCP(=O)(O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
46881751 13997 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 429 10 4 5 3.4 O=C(CCc1nc2ccccc2[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1085694 13997 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 429 10 4 5 3.4 O=C(CCc1nc2ccccc2[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
9947212 20380 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 364 9 3 5 1.2 CN(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL1194210 20380 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 364 9 3 5 1.2 CN(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL545742 20380 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 364 9 3 5 1.2 CN(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
44444172 101099 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 670 15 4 7 6.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(Cc1ccccc1)(Cc1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL250579 101099 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 670 15 4 7 6.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(Cc1ccccc1)(Cc1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.09.011
44335589 116165 0 None 74 2 Human 7.6 pEC50 = 7.6 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 540 15 4 7 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL321957 116165 0 None 74 2 Human 7.6 pEC50 = 7.6 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 540 15 4 7 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44268367 27609 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 344 9 4 5 1.9 CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13102 27609 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 344 9 4 5 1.9 CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
10291064 101255 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 341 8 2 6 2.9 O[C@@H](CNCCOc1ccc(-c2cscn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL251392 101255 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 341 8 2 6 2.9 O[C@@H](CNCCOc1ccc(-c2cscn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
46881840 15180 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.3 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
CHEMBL1093385 15180 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.3 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
CHEMBL1204416 15180 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 379 9 3 6 2.3 CC(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
44331444 11042 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 709 13 5 8 4.2 CC(C)N(Cc1cc(F)ccc1F)C(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
CHEMBL100589 11042 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 709 13 5 8 4.2 CC(C)N(Cc1cc(F)ccc1F)C(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
44312924 171605 0 None 39 3 Human 7.6 pEC50 = 7.6 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL421871 171605 0 None 39 3 Human 7.6 pEC50 = 7.6 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
76322043 112684 0 None -19 4 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
CHEMBL3128178 112684 0 None -19 4 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
45270697 201949 0 None -44 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203995 201949 0 None -44 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550444 201949 0 None -44 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45272417 202220 0 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448074 202220 0 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552368 202220 0 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10718924 117924 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 463 9 5 7 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32640 117924 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 463 9 5 7 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
44127171 185297 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466705 185297 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.bmc.2009.03.044
44444361 161521 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 401 8 2 5 4.7 O[C@@H](CNCCc1ccc(-c2csc(-c3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL399986 161521 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 401 8 2 5 4.7 O[C@@H](CNCCc1ccc(-c2csc(-c3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
15221055 211194 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
ChEMBL 368 9 3 5 3.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
CHEMBL72060 211194 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
ChEMBL 368 9 3 5 3.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
15221053 211375 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
ChEMBL 364 11 3 6 2.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL73220 211375 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
ChEMBL 364 11 3 6 2.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
11360474 99753 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 362 6 3 2 4.7 CC(Cc1c[nH]c2cc(Cl)ccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24414 99753 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 362 6 3 2 4.7 CC(Cc1c[nH]c2cc(Cl)ccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
24950564 181907 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 412 6 3 4 4.1 N#Cc1ccc([C@@H](O)CN[C@H]2CCc3ccc(-c4ccc(C(=O)O)cc4)cc3C2)cc1 10.1021/jm800222k
CHEMBL456972 181907 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 412 6 3 4 4.1 N#Cc1ccc([C@@H](O)CN[C@H]2CCc3ccc(-c4ccc(C(=O)O)cc4)cc3C2)cc1 10.1021/jm800222k
45272758 203153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 580 12 3 7 5.0 COc1ccc([C@@H](O)[C@H](C)NCCc2ccc(-c3ccc(C(=O)NS(C)(=O)=O)c(OC4CCCCC4)c3)cc2)cc1 10.1016/j.bmcl.2009.06.083
CHEMBL562596 203153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 580 12 3 7 5.0 COc1ccc([C@@H](O)[C@H](C)NCCc2ccc(-c3ccc(C(=O)NS(C)(=O)=O)c(OC4CCCCC4)c3)cc2)cc1 10.1016/j.bmcl.2009.06.083
16126657 143964 0 None -2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 573 14 4 8 4.2 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL374867 143964 0 None -2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 573 14 4 8 4.2 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCC3)c12 10.1016/j.bmcl.2006.08.010
44574826 185379 0 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1cn(Cc2ccccc2)cn1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467301 185379 0 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1cn(Cc2ccccc2)cn1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
45269866 202073 0 None -13 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448072 202073 0 None -13 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL551389 202073 0 None -13 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
46881750 13996 0 None 3 3 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 401 8 4 5 3.1 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1085693 13996 0 None 3 3 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 401 8 4 5 3.1 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
12043155 106518 0 None 34 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 14 3 8 4.8 CC(C)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL284965 106518 0 None 34 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 14 3 8 4.8 CC(C)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
24950405 179923 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1cccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL452129 179923 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1cccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
10145482 10942 0 None 34 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 604 12 5 7 3.4 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100057 10942 0 None 34 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 604 12 5 7 3.4 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
44281255 122272 0 None 69 3 Human 7.5 pEC50 = 7.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(OC(F)(F)F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33515 122272 0 None 69 3 Human 7.5 pEC50 = 7.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(OC(F)(F)F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
10136220 161603 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 409 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(C3CCCC3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL400392 161603 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 409 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(C3CCCC3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
44127171 185297 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL466705 185297 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44311597 211255 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 534 16 5 7 4.0 CCCCCCP(=O)(O)COc1ccc(CCNC[C@H](O)COc2ccc(O)c3c2CCC(=O)N3)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL72396 211255 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 534 16 5 7 4.0 CCCCCCP(=O)(O)COc1ccc(CCNC[C@H](O)COc2ccc(O)c3c2CCC(=O)N3)cc1 10.1016/S0960-894X(96)00603-8
44331553 11207 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 395 8 3 4 3.8 CC(C)N1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
CHEMBL101594 11207 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 395 8 3 4 3.8 CC(C)N1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
10209114 12253 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 540 17 5 7 4.2 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107591 12253 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 540 17 5 7 4.2 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
46881527 12364 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 375 8 3 4 3.5 Cc1ccccc1C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1077199 12364 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 375 8 3 4 3.5 Cc1ccccc1C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
10294264 16133 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 397 9 3 4 2.4 CN(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL111319 16133 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 397 9 3 4 2.4 CN(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(04)00462-7
3038500 16112 12 None -2 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL111201 16112 12 None -2 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/s0960-894x(04)00462-7
3038500 16112 12 None -2 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2007.06.072
CHEMBL111201 16112 12 None -2 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2007.06.072
44377726 63592 0 None 389 2 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 550 10 5 10 1.6 CS(=O)(=O)Nc1cc(O[C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
CHEMBL164378 63592 0 None 389 2 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 550 10 5 10 1.6 CS(=O)(=O)Nc1cc(O[C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
44396673 103562 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccccc4N)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL264819 103562 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccccc4N)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
101136737 68660 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 601 8 6 9 2.1 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(C)(=O)=O)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44386631 68660 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 601 8 6 9 2.1 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(C)(=O)=O)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
CHEMBL177400 68660 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 601 8 6 9 2.1 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(C)(=O)=O)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
146015362 7734 10 None -15 5 Rat 8.5 pEC50 = 8.5 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
3462 7734 10 None -15 5 Rat 8.5 pEC50 = 8.5 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
5486546 7734 10 None -15 5 Rat 8.5 pEC50 = 8.5 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
CHEMBL1204876 7734 10 None -15 5 Rat 8.5 pEC50 = 8.5 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
44281531 107298 0 None 3162 3 Human 8.5 pEC50 = 8.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 601 13 3 9 5.1 CSc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL291246 107298 0 None 3162 3 Human 8.5 pEC50 = 8.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 601 13 3 9 5.1 CSc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44281218 162490 0 None 501 3 Human 8.5 pEC50 = 8.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 645 13 5 9 4.0 CNC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL405245 162490 0 None 501 3 Human 8.5 pEC50 = 8.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 645 13 5 9 4.0 CNC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
127041870 143875 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 472 7 2 6 3.5 CCc1nnc([C@@H]2[C@H]3CN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)C[C@H]32)o1 10.1016/j.bmcl.2015.11.030
CHEMBL3747455 143875 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 472 7 2 6 3.5 CCc1nnc([C@@H]2[C@H]3CN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)C[C@H]32)o1 10.1016/j.bmcl.2015.11.030
24936491 24292 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257916 24292 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
24936763 24388 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 520 9 4 9 3.9 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258260 24388 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 520 9 4 9 3.9 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
42639133 19498 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187691 19498 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL515397 19498 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10416448 210172 0 None 1513 3 Human 8.5 pEC50 = 8.5 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 622 12 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL65461 210172 0 None 1513 3 Human 8.5 pEC50 = 8.5 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 622 12 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
1499 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
3779 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
536 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
CHEMBL434 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
DB01064 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
1499 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
3779 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
536 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
CHEMBL434 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
DB01064 8872 47 None -190 38 Human 8.5 pEC50 = 8.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
10217757 119047 0 None -10 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 119047 0 None -10 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
25071020 199964 0 None 1 3 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 11 3 5 5.5 CC(C)Oc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL523265 199964 0 None 1 3 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 11 3 5 5.5 CC(C)Oc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
16222940 193253 0 None -48 4 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL487682 193253 0 None -48 4 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44591507 186138 0 None -48 4 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473702 186138 0 None -48 4 Dog 8.5 pEC50 = 8.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
24950061 194739 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 480 8 3 5 5.1 CN(C)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL497113 194739 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 480 8 3 5 5.1 CN(C)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
24949564 196300 0 None 147 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 452 7 4 5 4.6 Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL514094 196300 0 None 147 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 452 7 4 5 4.6 Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
44392534 72012 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 443 11 4 6 3.4 C=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182689 72012 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 443 11 4 6 3.4 C=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44298516 202368 0 None 275 3 Human 8.5 pEC50 = 8.5 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 467 8 1 5 6.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1nc(CCCC2CCCC2)cs1 10.1016/s0960-894x(99)00277-2
CHEMBL55541 202368 0 None 275 3 Human 8.5 pEC50 = 8.5 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 467 8 1 5 6.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1nc(CCCC2CCCC2)cs1 10.1016/s0960-894x(99)00277-2
67972106 143866 0 None 1698 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 448 5 2 5 3.3 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCC2(CCOC2=O)CC1 10.1016/j.bmcl.2015.11.030
CHEMBL3747244 143866 0 None 1698 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 448 5 2 5 3.3 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCC2(CCOC2=O)CC1 10.1016/j.bmcl.2015.11.030
44307085 109601 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 588 12 4 9 3.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(C(O)c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL305476 109601 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 588 12 4 9 3.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(C(O)c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
24812042 162202 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 343 9 3 4 2.8 CC(C)(Oc1ccc(CCNC[C@@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL403711 162202 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 343 9 3 4 2.8 CC(C)(Oc1ccc(CCNC[C@@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
25071020 199964 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 11 3 5 5.5 CC(C)Oc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL523265 199964 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 11 3 5 5.5 CC(C)Oc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44461718 212642 0 None 97 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
44461718 212642 0 None 97 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL83753 212642 0 None 97 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
CHEMBL83753 212642 0 None 97 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
145983266 172307 0 None 66 3 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 512 14 5 6 2.7 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4241176 172307 0 None 66 3 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 512 14 5 6 2.7 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
24949722 182310 0 None 223 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 6 3 3 5.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(C(F)(F)F)cc2)CC3)cc1 10.1021/jm800222k
CHEMBL457839 182310 0 None 223 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 6 3 3 5.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(C(F)(F)F)cc2)CC3)cc1 10.1021/jm800222k
44472610 144735 0 None 1 4 Rhesus macaque 8.5 pEC50 = 8.5 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764088 144735 0 None 1 4 Rhesus macaque 8.5 pEC50 = 8.5 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
145984667 172168 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 462 10 5 4 4.5 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)Nc1ccccc1F 10.1016/j.ejmech.2018.03.032
CHEMBL4237902 172168 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 462 10 5 4 4.5 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)Nc1ccccc1F 10.1016/j.ejmech.2018.03.032
10437614 107719 12 None 30 3 Human 8.4 pEC50 = 8.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL294042 107719 12 None 30 3 Human 8.4 pEC50 = 8.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00571-x
24950242 195419 0 None 12 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 8 3 6 4.4 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1C(=O)O 10.1021/jm800222k
CHEMBL503209 195419 0 None 12 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 8 3 6 4.4 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1C(=O)O 10.1021/jm800222k
3038500 16112 12 None -2 6 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL111201 16112 12 None -2 6 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.01.130
10437614 107719 12 None 30 3 Human 8.4 pEC50 = 8.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL294042 107719 12 None 30 3 Human 8.4 pEC50 = 8.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
3038500 16112 12 None -2 6 Human 8.4 pEC50 = 8.4 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL111201 16112 12 None -2 6 Human 8.4 pEC50 = 8.4 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
11476004 180272 0 None -4 3 Dog 8.4 pEC50 = 8.4 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453047 180272 0 None -4 3 Dog 8.4 pEC50 = 8.4 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
70792359 112694 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
CHEMBL3128188 112694 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
127042536 143771 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)C1CCc2ccnn21 10.1016/j.bmcl.2015.11.030
CHEMBL3745911 143771 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)C1CCc2ccnn21 10.1016/j.bmcl.2015.11.030
70792359 112694 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/acs.jmedchem.5b01372
CHEMBL3128188 112694 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/acs.jmedchem.5b01372
44298821 201774 0 None 47 3 Human 8.4 pEC50 = 8.4 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 453 11 1 5 6.1 CCCCCCCCc1cnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)o1 10.1016/s0960-894x(99)00277-2
CHEMBL54749 201774 0 None 47 3 Human 8.4 pEC50 = 8.4 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 453 11 1 5 6.1 CCCCCCCCc1cnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)o1 10.1016/s0960-894x(99)00277-2
24812154 102811 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 CC(Oc1ccc(CCNCC(O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL259858 102811 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 329 9 3 4 2.4 CC(Oc1ccc(CCNCC(O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
11810992 32880 0 None 1698 3 Human 8.4 pEC50 = 8.4 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL13560 32880 0 None 1698 3 Human 8.4 pEC50 = 8.4 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
44307144 210388 0 None 112 3 Human 8.4 pEC50 = 8.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 569 17 5 7 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL67015 210388 0 None 112 3 Human 8.4 pEC50 = 8.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 569 17 5 7 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
11810992 32880 0 None 1698 3 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL13560 32880 0 None 1698 3 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
24812041 102900 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 343 9 3 4 2.8 CC(C)(Oc1ccc(CCNC[C@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL260393 102900 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 343 9 3 4 2.8 CC(C)(Oc1ccc(CCNC[C@H](O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
1499 8872 47 None -190 38 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
3779 8872 47 None -190 38 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
536 8872 47 None -190 38 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
CHEMBL434 8872 47 None -190 38 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
DB01064 8872 47 None -190 38 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
44472592 144811 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1cnccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764950 144811 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1cnccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
9512 10408 42 None 380 3 Human 8.4 pEC50 = 8.4 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
9887812 10408 42 None 380 3 Human 8.4 pEC50 = 8.4 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
CHEMBL208427 10408 42 None 380 3 Human 8.4 pEC50 = 8.4 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
DB06190 10408 42 None 380 3 Human 8.4 pEC50 = 8.4 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
44441233 154835 0 None 79 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2ocnc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393471 154835 0 None 79 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2ocnc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44268322 25744 0 None 5 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 303 8 4 5 1.7 Oc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12876 25744 0 None 5 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 303 8 4 5 1.7 Oc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
9803988 207125 1 None -1 2 Dog 7.5 pEC50 = 7.5 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm701324c
9803988 207125 1 None -1 2 Dog 7.5 pEC50 = 7.5 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm800222k
CHEMBL59765 207125 1 None -1 2 Dog 7.5 pEC50 = 7.5 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm701324c
CHEMBL59765 207125 1 None -1 2 Dog 7.5 pEC50 = 7.5 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm800222k
9803988 207125 1 None -1 2 Dog 7.5 pEC50 = 7.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm8000345
CHEMBL59765 207125 1 None -1 2 Dog 7.5 pEC50 = 7.5 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 417 8 2 5 3.9 CCOC(=O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC2 10.1021/jm8000345
44219641 185218 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 3 6 4.1 CC(Cc1ccc(NC(=O)Cc2nccn2Cc2ccccc2)cc1)NC[C@H](O)COc1ccccc1 10.1016/j.bmc.2009.03.044
CHEMBL466088 185218 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 3 6 4.1 CC(Cc1ccc(NC(=O)Cc2nccn2Cc2ccccc2)cc1)NC[C@H](O)COc1ccccc1 10.1016/j.bmc.2009.03.044
24895194 185925 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 512 12 4 6 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL472105 185925 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 512 12 4 6 4.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44309523 108966 0 None 30 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 420 10 3 6 2.3 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)cc3)C2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL302803 108966 0 None 30 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 420 10 3 6 2.3 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)cc3)C2)cc1 10.1016/s0960-894x(03)00387-1
44458134 91608 0 None 109 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 565 15 3 10 3.1 CCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
CHEMBL22345 91608 0 None 109 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 565 15 3 10 3.1 CCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
44306979 210474 0 None 33 3 Human 7.5 pEC50 = 7.5 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 476 11 4 7 2.7 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67534 210474 0 None 33 3 Human 7.5 pEC50 = 7.5 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 476 11 4 7 2.7 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44336180 13241 0 None 15 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1ccc(F)cc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL108263 13241 0 None 15 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1ccc(F)cc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10202842 170938 0 None 16 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 428 10 5 6 1.9 NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL421030 170938 0 None 16 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 428 10 5 6 1.9 NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44331530 11194 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 604 17 5 7 4.6 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c(C)c3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL101520 11194 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 604 17 5 7 4.6 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c(C)c3)CC2)cc1 10.1016/s0960-894x(02)00607-8
10131985 161419 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 339 8 2 6 2.7 Cc1ocnc1-c1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2007.06.072
CHEMBL399440 161419 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 339 8 2 6 2.7 Cc1ocnc1-c1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2007.06.072
1028 7079 71 None -4 19 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
139148732 7079 71 None -4 19 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
479 7079 71 None -4 19 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
5816 7079 71 None -4 19 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
CHEMBL679 7079 71 None -4 19 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
DB00668 7079 71 None -4 19 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
44580042 199878 0 None 26 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 396 9 3 5 3.6 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
CHEMBL522641 199878 0 None 26 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 396 9 3 5 3.6 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
44331443 11221 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 689 14 7 9 2.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101674 11221 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 689 14 7 9 2.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44331351 214920 0 None 16 3 Human 7.5 pEC50 = 7.5 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 610 13 6 8 2.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL98088 214920 0 None 16 3 Human 7.5 pEC50 = 7.5 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 610 13 6 8 2.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44298315 200077 0 None 3 3 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 454 11 1 6 5.5 CCCCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
CHEMBL52407 200077 0 None 3 3 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 454 11 1 6 5.5 CCCCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
44281344 106620 0 None 64 3 Human 7.5 pEC50 = 7.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 628 14 4 10 4.3 CC(=O)Nc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285704 106620 0 None 64 3 Human 7.5 pEC50 = 7.5 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 628 14 4 10 4.3 CC(=O)Nc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
11495581 84097 0 None 25 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 425 9 4 5 4.2 C[C@H](CNc1cccc(-c2ncccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL208328 84097 0 None 25 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 425 9 4 5 4.2 C[C@H](CNc1cccc(-c2ncccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
11546349 148111 0 None 25 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL383511 148111 0 None 25 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
56678845 73180 0 None -15 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
CHEMBL1814269 73180 0 None -15 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
CHEMBL1851839 73180 0 None -15 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
56943517 119281 0 None -15 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
CHEMBL3298832 119281 0 None -15 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
56672269 73361 0 None -50 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835858 73361 0 None -50 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852564 73361 0 None -50 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
10203169 21011 0 None -39 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1086536 21011 0 None -39 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1199300 21011 0 None -39 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
44574722 185331 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 433 11 3 5 3.5 Cc1cc(C)nc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.03.044
CHEMBL466925 185331 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 433 11 3 5 3.5 Cc1cc(C)nc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.03.044
45273268 202408 0 None -194 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204004 202408 0 None -194 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL556274 202408 0 None -194 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
24936625 24256 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 520 9 4 9 3.8 O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257798 24256 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 520 9 4 9 3.8 O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
44369602 53616 0 None -6 2 Human 6.5 pEC50 = 6.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1cccc(CC(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154036 53616 0 None -6 2 Human 6.5 pEC50 = 6.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1cccc(CC(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
56658244 73182 0 None -125 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814272 73182 0 None -125 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851849 73182 0 None -125 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
42625517 19493 0 None -630 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187654 19493 0 None -630 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL514032 19493 0 None -630 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625898 192034 0 None -125 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL485847 192034 0 None -125 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46832507 20986 0 None -199 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085638 20986 0 None -199 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198915 20986 0 None -199 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
44331791 114768 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 423 11 3 4 4.6 CCCCCN1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
CHEMBL319406 114768 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 423 11 3 4 4.6 CCCCCN1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
44280860 106690 0 None 204 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 521 13 3 8 4.1 CCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL286139 106690 0 None 204 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 521 13 3 8 4.1 CCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
24822970 164899 0 None 9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 9 3 3 4.5 O=C(O)Cc1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL408694 164899 0 None 9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 9 3 3 4.5 O=C(O)Cc1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
46881982 12524 0 None 53 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCc1ccccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078465 12524 0 None 53 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCc1ccccc1 10.1016/j.bmcl.2010.01.130
44392569 73018 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 544 11 3 8 3.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(OS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL184584 73018 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 544 11 3 8 3.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(OS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44307379 210425 0 None 23 3 Human 7.5 pEC50 = 7.5 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 427 11 3 6 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00381-3
CHEMBL67251 210425 0 None 23 3 Human 7.5 pEC50 = 7.5 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 427 11 3 6 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00381-3
44307378 210579 0 None 15 3 Human 7.5 pEC50 = 7.5 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 478 11 3 7 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00381-3
CHEMBL68334 210579 0 None 15 3 Human 7.5 pEC50 = 7.5 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 478 11 3 7 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00381-3
10302915 12120 0 None 23 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1c(F)cccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL106884 12120 0 None 23 2 Human 7.5 pEC50 = 7.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1c(F)cccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
45269025 202926 0 None -39 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203991 202926 0 None -39 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL561173 202926 0 None -39 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
24823782 104821 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 396 8 3 4 4.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
CHEMBL273097 104821 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 396 8 3 4 4.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
24950566 182312 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 6 3 3 5.5 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)c(Cl)c2)CC3)cc1 10.1021/jm800222k
CHEMBL457840 182312 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 6 3 3 5.5 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)c(Cl)c2)CC3)cc1 10.1021/jm800222k
24937016 24529 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258706 24529 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
11381882 106078 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL282039 106078 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
44402823 77040 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 597 14 3 6 6.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(CCc3ccccc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL194168 77040 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 597 14 3 6 6.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(CCc3ccccc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44402838 179242 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 633 13 3 6 7.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL448158 179242 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 633 13 3 6 7.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301843 206387 0 None 27 3 Human 7.5 pEC50 = 7.5 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 584 13 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCc3ccccc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL59270 206387 0 None 27 3 Human 7.5 pEC50 = 7.5 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 584 13 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCc3ccccc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
45271492 202013 0 None -16 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203997 202013 0 None -16 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL550906 202013 0 None -16 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
11381882 106078 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL282039 106078 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
45273276 202463 0 None -141 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204005 202463 0 None -141 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL556689 202463 0 None -141 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
122184833 129315 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 446 9 4 6 2.9 CC(C)(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601306 129315 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 446 9 4 6 2.9 CC(C)(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
135995976 67001 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 514 8 6 9 0.8 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(/C=C4\N=C(N)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL174054 67001 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 514 8 6 9 0.8 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(/C=C4\N=C(N)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
9894801 127515 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 592 11 5 10 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)N(CC(=O)O)C4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL354906 127515 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 592 11 5 10 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)N(CC(=O)O)C4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
44285226 106624 0 None 35 3 Human 7.5 pEC50 = 7.5 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 548 15 3 7 5.5 CCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL285713 106624 0 None 35 3 Human 7.5 pEC50 = 7.5 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 548 15 3 7 5.5 CCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
45270690 201900 0 None -19 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203994 201900 0 None -19 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550037 201900 0 None -19 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45267257 203461 0 None -41 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203987 203461 0 None -41 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL564648 203461 0 None -41 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
3038500 16112 12 None -1258 6 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 16112 12 None -1258 6 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
44281276 106594 0 None 28 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 15 3 8 4.9 CCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL285481 106594 0 None 28 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 15 3 8 4.9 CCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
52943932 24528 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 485 8 2 8 4.2 N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258705 24528 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 485 8 2 8 4.2 N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
46881983 12539 0 None 48 2 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 477 9 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1078575 12539 0 None 48 2 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 477 9 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
12017003 148708 0 None 87 3 Human 7.5 pEC50 = 7.5 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38704 148708 0 None 87 3 Human 7.5 pEC50 = 7.5 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
12017007 165157 0 None 54 3 Human 7.5 pEC50 = 7.5 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL40898 165157 0 None 54 3 Human 7.5 pEC50 = 7.5 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
10112753 19808 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 418 9 3 5 2.3 CC1CCN(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL1189942 19808 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 418 9 3 5 2.3 CC1CCN(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL539799 19808 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 418 9 3 5 2.3 CC1CCN(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
10188669 172107 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 588 14 6 8 3.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL423491 172107 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 588 14 6 8 3.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(03)00387-1
46881937 13536 0 None 138 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 494 9 3 6 5.5 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2s1 10.1016/j.bmcl.2010.01.130
CHEMBL1083831 13536 0 None 138 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 494 9 3 6 5.5 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2s1 10.1016/j.bmcl.2010.01.130
44392558 72029 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182770 72029 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
10140889 12838 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 484 12 4 6 3.3 CCN(CC)C(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL108061 12838 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 484 12 4 6 3.3 CCN(CC)C(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10745501 117326 0 None 288 2 Human 7.4 pEC50 = 7.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 562 13 5 8 2.4 CCCCN(CC(=O)O)C(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL32521 117326 0 None 288 2 Human 7.4 pEC50 = 7.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 562 13 5 8 2.4 CCCCN(CC(=O)O)C(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
44127052 202515 0 None 2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccccc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL557269 202515 0 None 2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccccc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44309320 211419 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 527 12 4 8 2.0 CCCCOc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)C2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL73557 211419 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 527 12 4 8 2.0 CCCCOc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)C2)cc1 10.1016/s0960-894x(03)00387-1
44313150 110554 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308868 110554 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
9967732 100939 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 339 8 2 6 2.7 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL249534 100939 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 339 8 2 6 2.7 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
24949887 194932 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
CHEMBL498519 194932 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
44377957 64275 0 None 141 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 537 13 3 6 3.8 CCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL166013 64275 0 None 141 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 537 13 3 6 3.8 CCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
46882031 12567 0 None 10 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078749 12567 0 None 10 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2010.01.130
46845697 14520 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 410 9 3 6 3.2 Cc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c(C)s1 10.1016/j.bmcl.2010.01.130
CHEMBL1089053 14520 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 410 9 3 6 3.2 Cc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c(C)s1 10.1016/j.bmcl.2010.01.130
10119515 115166 0 None 7 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL319840 115166 0 None 7 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
12017002 148477 0 None 173 3 Human 7.4 pEC50 = 7.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 558 11 3 7 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)cc3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38562 148477 0 None 173 3 Human 7.4 pEC50 = 7.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 558 11 3 7 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)cc3)o2)cc1 10.1016/s0960-894x(00)00277-8
45271518 201863 0 None -25 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203999 201863 0 None -25 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL549689 201863 0 None -25 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
46881869 14870 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 393 9 3 6 2.5 CC(C)(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
CHEMBL1091478 14870 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 393 9 3 6 2.5 CC(C)(C(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)n1cccn1 10.1016/j.bmcl.2010.01.130
44335498 114320 0 None 26 3 Human 7.4 pEC50 = 7.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 447 9 3 5 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00571-x
CHEMBL318802 114320 0 None 26 3 Human 7.4 pEC50 = 7.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 447 9 3 5 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00571-x
11189002 100840 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 406 6 3 2 4.8 CC(Cc1c[nH]c2cc(Br)ccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24899 100840 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 406 6 3 2 4.8 CC(Cc1c[nH]c2cc(Br)ccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
10200545 20640 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 392 9 3 5 1.9 CN(C)S(=O)(=O)Nc1ccc(CC(C)(C)NC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL1196004 20640 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 392 9 3 5 1.9 CN(C)S(=O)(=O)Nc1ccc(CC(C)(C)NC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL555764 20640 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 392 9 3 5 1.9 CN(C)S(=O)(=O)Nc1ccc(CC(C)(C)NC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
24950560 179523 0 None 16 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccccc2Cl)CC3)cc1 10.1021/jm800222k
CHEMBL450842 179523 0 None 16 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccccc2Cl)CC3)cc1 10.1021/jm800222k
44392212 175148 0 None -12 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204383 175148 0 None -12 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL434524 175148 0 None -12 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44377485 126785 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 612 11 5 10 3.0 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4ccc(O)c(NS(=O)(=O)c5ccccc5)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL350131 126785 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 612 11 5 10 3.0 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4ccc(O)c(NS(=O)(=O)c5ccccc5)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
10230721 119177 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 543 9 3 5 4.9 O=S(=O)(c1ccc2ccccc2c1)N1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
CHEMBL329729 119177 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 543 9 3 5 4.9 O=S(=O)(c1ccc2ccccc2c1)N1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
46889854 14080 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086077 14080 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
44268349 27348 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 456 12 4 6 2.9 O=S(=O)(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13079 27348 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 456 12 4 6 2.9 O=S(=O)(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44281277 106954 0 None 36 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 563 16 3 8 5.3 CCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL288083 106954 0 None 36 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 563 16 3 8 5.3 CCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
127037832 144830 0 None -16 4 Dog 7.4 pEC50 = 7.4 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None -16 4 Dog 7.4 pEC50 = 7.4 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
24824226 104218 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 439 11 3 4 4.3 O=C(O)COc1ccc(Cc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL270027 104218 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 439 11 3 4 4.3 O=C(O)COc1ccc(Cc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
24824352 165941 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
CHEMBL409828 165941 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
24824352 165941 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1016/j.bmcl.2008.08.009
CHEMBL409828 165941 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1016/j.bmcl.2008.08.009
24824352 165941 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm800222k
CHEMBL409828 165941 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1cccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm800222k
9842600 194895 0 None 38 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 375 7 3 4 3.0 O=C(O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
CHEMBL498305 194895 0 None 38 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 375 7 3 4 3.0 O=C(O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
12017001 153823 0 None 77 3 Human 7.4 pEC50 = 7.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 540 11 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccccc3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL39269 153823 0 None 77 3 Human 7.4 pEC50 = 7.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 540 11 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccccc3)o2)cc1 10.1016/s0960-894x(00)00277-8
10648298 106495 0 None 120 3 Human 7.4 pEC50 = 7.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 477 10 5 7 2.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284788 106495 0 None 120 3 Human 7.4 pEC50 = 7.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 477 10 5 7 2.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
11718543 172611 0 None 125 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)n1 10.1021/jm0509445
CHEMBL424866 172611 0 None 125 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)n1 10.1021/jm0509445
1499 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
3779 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
536 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
CHEMBL434 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
DB01064 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
56675511 73183 0 None -31 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814273 73183 0 None -31 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1851850 73183 0 None -31 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
9892481 77008 14 None -794 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 77008 14 None -794 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
56943515 119221 0 None -44 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298213 119221 0 None -44 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
66796015 119237 0 None -177 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298328 119237 0 None -177 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943518 119238 0 None -125 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298329 119238 0 None -125 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943545 119239 0 None -141 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298330 119239 0 None -141 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943546 119255 0 None -125 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298691 119255 0 None -125 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
11180293 119285 0 None -89 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 119285 0 None -89 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
1499 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
3779 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
536 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
CHEMBL434 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
DB01064 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
10288976 73354 0 None -251 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835862 73354 0 None -251 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852543 73354 0 None -251 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
1499 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
3779 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
536 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
CHEMBL434 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
DB01064 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
1499 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
3779 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
536 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
CHEMBL434 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
DB01064 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
46832505 21007 1 None -15 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
CHEMBL1085395 21007 1 None -15 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
CHEMBL1199261 21007 1 None -15 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
44574721 185330 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 419 11 3 5 3.1 Cc1cccnc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466924 185330 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 419 11 3 5 3.1 Cc1cccnc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
56658246 71271 0 None -1995 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814277 71271 0 None -1995 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814278 71271 0 None -1995 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
46832804 13758 0 None -199 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1084655 13758 0 None -199 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
10183066 20039 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 460 9 3 5 3.4 C[C@H]1C[C@@H](C)CN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)C1 10.1016/s0960-894x(04)00462-7
CHEMBL1191579 20039 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 460 9 3 5 3.4 C[C@H]1C[C@@H](C)CN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)C1 10.1016/s0960-894x(04)00462-7
CHEMBL542696 20039 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 460 9 3 5 3.4 C[C@H]1C[C@@H](C)CN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)C1 10.1016/s0960-894x(04)00462-7
24823462 104486 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 461 10 3 5 4.5 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCOCC1 10.1021/jm701324c
CHEMBL271401 104486 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 461 10 3 5 4.5 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCOCC1 10.1021/jm701324c
44313090 109947 0 None 75 3 Human 8.4 pEC50 = 8.4 Functional
Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nMCompound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
ChEMBL 568 12 6 7 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(OCC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308126 109947 0 None 75 3 Human 8.4 pEC50 = 8.4 Functional
Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nMCompound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
ChEMBL 568 12 6 7 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(OCC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
12017011 107141 0 None 158 3 Human 8.4 pEC50 = 8.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL289689 107141 0 None 158 3 Human 8.4 pEC50 = 8.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
10651147 117460 0 None 380 3 Human 8.4 pEC50 = 8.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32599 117460 0 None 380 3 Human 8.4 pEC50 = 8.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
10393774 127521 0 None 501 3 Human 8.4 pEC50 = 8.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 598 14 5 9 2.1 CCCCN(c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)S(=O)(=O)CC(=O)O 10.1021/jm000544b
CHEMBL35500 127521 0 None 501 3 Human 8.4 pEC50 = 8.4 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 598 14 5 9 2.1 CCCCN(c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)S(=O)(=O)CC(=O)O 10.1021/jm000544b
44281396 106735 0 None 123 3 Human 8.4 pEC50 = 8.4 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286435 106735 0 None 123 3 Human 8.4 pEC50 = 8.4 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44281400 117136 0 None 363 3 Human 8.4 pEC50 = 8.4 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL32411 117136 0 None 363 3 Human 8.4 pEC50 = 8.4 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
51346867 65433 0 None 537 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684583 65433 0 None 537 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
24949572 183805 0 None 34 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)c1 10.1021/jm800222k
CHEMBL463182 183805 0 None 34 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)c1 10.1021/jm800222k
12049922 109518 0 None 208 3 Human 8.4 pEC50 = 8.4 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 638 13 3 9 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL304991 109518 0 None 208 3 Human 8.4 pEC50 = 8.4 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 638 13 3 9 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
15523861 64299 0 None 478 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 599 14 3 6 4.6 O=C1N(CCCc2ccccc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL166188 64299 0 None 478 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 599 14 3 6 4.6 O=C1N(CCCc2ccccc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44268308 24881 0 None 33 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 472 12 4 7 2.8 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12686 24881 0 None 33 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 472 12 4 7 2.8 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
44472613 144783 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 417 7 3 5 2.9 O=C(Cn1ccccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764592 144783 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 417 7 3 5 2.9 O=C(Cn1ccccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
24823134 104176 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 449 13 3 5 4.3 CCOCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL269816 104176 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 449 13 3 5 4.3 CCOCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
44396521 130458 0 None 6 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 514 12 5 7 3.6 C[C@H](Cc1c[nH]c2c(OCCN)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL362136 130458 0 None 6 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 514 12 5 7 3.6 C[C@H](Cc1c[nH]c2c(OCCN)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
12017012 106598 0 None 72 3 Human 8.4 pEC50 = 8.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 622 12 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL285520 106598 0 None 72 3 Human 8.4 pEC50 = 8.4 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 622 12 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
10722793 120124 0 None 114 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL331744 120124 0 None 114 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
44377637 62305 0 None 457 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 633 14 3 6 5.3 O=C1N(CCCc2ccc(Cl)cc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL162043 62305 0 None 457 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 633 14 3 6 5.3 O=C1N(CCCc2ccc(Cl)cc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
24949889 194934 0 None 35 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CCC3)c1 10.1021/jm800222k
CHEMBL498531 194934 0 None 35 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CCC3)c1 10.1021/jm800222k
145984042 172454 0 None 1348 3 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 475 13 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Cc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4244929 172454 0 None 1348 3 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 475 13 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Cc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
24823624 165940 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL409827 165940 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
44580040 193899 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 510 10 4 5 5.7 CC(C)(C)C(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL491645 193899 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 510 10 4 5 5.7 CC(C)(C)C(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44268497 25718 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1cccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)c1 10.1016/s0960-894x(98)00170-x
CHEMBL12864 25718 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1cccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)c1 10.1016/s0960-894x(98)00170-x
145982519 172212 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 474 11 5 5 4.4 COc1cccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4238856 172212 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 474 11 5 5 4.4 COc1cccc(NC(=O)Nc2ccc(CCNC[C@H](O)COc3cccc4[nH]ccc34)cc2)c1 10.1016/j.ejmech.2018.03.032
145983711 172162 0 None 2089 3 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 476 12 5 5 3.5 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4237802 172162 0 None 2089 3 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 476 12 5 5 3.5 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
24949570 181837 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1C(=O)O 10.1021/jm800222k
CHEMBL456795 181837 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1C(=O)O 10.1021/jm800222k
52943362 24320 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 466 8 2 8 4.4 OC(CNC1CCN(c2ncnc3scc(-c4cccs4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258025 24320 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 466 8 2 8 4.4 OC(CNC1CCN(c2ncnc3scc(-c4cccs4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
70792359 112694 0 None -1 4 Rhesus macaque 8.3 pEC50 = 8.3 Functional
Agonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
CHEMBL3128188 112694 0 None -1 4 Rhesus macaque 8.3 pEC50 = 8.3 Functional
Agonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rhesus monkey beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
44268324 23556 0 None 58 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12450 23556 0 None 58 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00169-3
44472610 144735 0 None -1 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764088 144735 0 None -1 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
10048077 104670 17 None 52 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272383 104670 17 None 52 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
24950238 181733 0 None 69 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c1 10.1021/jm800222k
CHEMBL456578 181733 0 None 69 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c1 10.1021/jm800222k
10048077 104670 17 None 52 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL272383 104670 17 None 52 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
10048077 104670 17 None 52 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL272383 104670 17 None 52 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
42639133 19498 0 None -1 2 Dog 8.3 pEC50 = 8.3 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187691 19498 0 None -1 2 Dog 8.3 pEC50 = 8.3 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL515397 19498 0 None -1 2 Dog 8.3 pEC50 = 8.3 Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 3 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
24812040 102899 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 343 9 3 4 2.8 CC(C)(Oc1ccc(CCNCC(O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
CHEMBL260392 102899 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 343 9 3 4 2.8 CC(C)(Oc1ccc(CCNCC(O)c2ccccc2)cc1)C(=O)O 10.1016/j.bmc.2007.11.060
24822643 164433 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(F)c1 10.1021/jm701324c
CHEMBL408145 164433 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(F)c1 10.1021/jm701324c
44461705 212634 0 None 75 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL83698 212634 0 None 75 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
44392255 172740 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 401 11 5 5 2.1 CC(C)NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL425173 172740 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 401 11 5 5 2.1 CC(C)NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44302005 107337 0 None 6165 3 Human 8.3 pEC50 = 8.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 595 11 4 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3c[nH]c4ccccc34)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL291516 107337 0 None 6165 3 Human 8.3 pEC50 = 8.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 595 11 4 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3c[nH]c4ccccc34)cs2)cc1 10.1016/s0960-894x(00)00390-5
10180440 129297 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601201 129297 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
10139127 64263 0 None 50 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 455 9 3 7 2.6 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL165893 64263 0 None 50 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 455 9 3 7 2.6 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44402729 140389 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 570 12 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cccnc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL371334 140389 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 570 12 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cccnc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301805 107793 0 None 75 3 Human 7.4 pEC50 = 7.4 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccnc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL294492 107793 0 None 75 3 Human 7.4 pEC50 = 7.4 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccnc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
45273281 202517 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448075 202517 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL557295 202517 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
44311779 109651 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 410 11 4 7 1.3 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL305808 109651 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 410 11 4 7 1.3 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/S0960-894X(96)00603-8
101136735 138234 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 538 8 5 8 2.4 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44386136 138234 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 538 8 5 8 2.4 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
88054179 138234 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 538 8 5 8 2.4 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
CHEMBL369155 138234 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 538 8 5 8 2.4 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44306992 210540 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 442 11 4 7 2.0 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67993 210540 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 442 11 4 7 2.0 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44268281 23650 0 None -15 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 436 14 4 6 2.9 CCCCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12498 23650 0 None -15 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 436 14 4 6 2.9 CCCCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
10182229 20131 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 447 9 3 6 1.6 CN1CCN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL1192404 20131 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 447 9 3 6 1.6 CN1CCN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
CHEMBL543633 20131 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 447 9 3 6 1.6 CN1CCN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)CC1 10.1016/s0960-894x(04)00462-7
52947443 24386 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(F)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258258 24386 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(F)c1 10.1016/j.bmcl.2010.08.039
10280301 116514 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccc(F)cc1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL322973 116514 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccc(F)cc1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
45269853 203347 0 None 4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL563872 203347 0 None 4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
9924779 101215 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 355 9 3 7 1.9 OCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL251180 101215 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 355 9 3 7 1.9 OCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
46881938 13537 0 None 72 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 9 3 4 5.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1C1CCCCC1 10.1016/j.bmcl.2010.01.130
CHEMBL1083832 13537 0 None 72 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 9 3 4 5.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1C1CCCCC1 10.1016/j.bmcl.2010.01.130
14823035 148341 2 None -26 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
CHEMBL38486 148341 2 None -26 4 Human 6.4 pEC50 = 6.4 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
122184772 129299 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601203 129299 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
10121328 11210 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101606 11210 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44307196 210366 0 None 8 3 Human 7.4 pEC50 = 7.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 510 11 4 7 3.3 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL66859 210366 0 None 8 3 Human 7.4 pEC50 = 7.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 510 11 4 7 3.3 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44306991 210461 0 None 30 3 Human 7.4 pEC50 = 7.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 493 11 4 8 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3cnc4ccccc4c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67461 210461 0 None 30 3 Human 7.4 pEC50 = 7.4 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 493 11 4 8 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3cnc4ccccc4c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
70792359 112694 0 None -117 4 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
CHEMBL3128188 112694 0 None -117 4 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 417 6 3 6 2.8 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2ccnn21 10.1021/jm4017224
76322046 112701 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
CHEMBL3128195 112701 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 448 6 4 6 3.8 Nc1nc2c(s1)CC[C@@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/jm4017224
44268254 26785 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 302 8 4 5 1.5 Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13034 26785 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 302 8 4 5 1.5 Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
45270680 201817 0 None -5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203993 201817 0 None -5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549421 201817 0 None -5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
44444365 101033 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 393 7 2 5 4.1 O[C@@H](CNCCc1ccc(-c2csc(C(F)(F)F)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250184 101033 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 393 7 2 5 4.1 O[C@@H](CNCCc1ccc(-c2csc(C(F)(F)F)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
44402734 141969 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 585 12 4 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc(O)cc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL372056 141969 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 585 12 4 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc(O)cc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44402735 175252 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 626 13 4 7 6.0 CC(=O)Nc1ccc(-c2csc(Cc3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5ccccc5)cc4)cc3)n2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL435134 175252 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 626 13 4 7 6.0 CC(=O)Nc1ccc(-c2csc(Cc3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5ccccc5)cc4)cc3)n2)cc1 10.1016/j.bmcl.2005.03.119
10304565 114154 0 None 11 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 622 12 5 7 3.6 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c(F)c3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL317809 114154 0 None 11 2 Human 7.4 pEC50 = 7.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 622 12 5 7 3.6 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c(F)c3)CC2)cc1 10.1016/s0960-894x(02)00607-8
44301867 107352 0 None 21 3 Human 7.4 pEC50 = 7.4 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 613 12 4 8 5.5 CC(=O)Nc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL291594 107352 0 None 21 3 Human 7.4 pEC50 = 7.4 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 613 12 4 8 5.5 CC(=O)Nc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
44301818 209529 0 None 24 3 Human 7.4 pEC50 = 7.4 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 572 11 4 8 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(O)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL61962 209529 0 None 24 3 Human 7.4 pEC50 = 7.4 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 572 11 4 8 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(O)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
567 7512 16 None -2 7 Human 6.4 pEC50 = 6.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
9841972 7512 16 None -2 7 Human 6.4 pEC50 = 6.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
CHEMBL284782 7512 16 None -2 7 Human 6.4 pEC50 = 6.4 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
45270690 201900 0 None -19 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203994 201900 0 None -19 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550037 201900 0 None -19 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45268136 203164 0 None -7 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203989 203164 0 None -7 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL562669 203164 0 None -7 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
567 7512 16 None -2 7 Human 6.4 pEC50 = 6.4 Functional
Compound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonistCompound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonist
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
9841972 7512 16 None -2 7 Human 6.4 pEC50 = 6.4 Functional
Compound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonistCompound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonist
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
CHEMBL284782 7512 16 None -2 7 Human 6.4 pEC50 = 6.4 Functional
Compound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonistCompound was evaluated for agonistic activity in human Beta-3 adrenergic receptor assay; partial weak agonist
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
46881753 14037 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 10 3 6 3.4 Cn1c(CCC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)nc2ccccc21 10.1016/j.bmcl.2010.01.130
CHEMBL1085929 14037 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 443 10 3 6 3.4 Cn1c(CCC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)nc2ccccc21 10.1016/j.bmcl.2010.01.130
10787873 106649 0 None 3 2 Rat 6.3 pEC50 = 6.3 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL285888 106649 0 None 3 2 Rat 6.3 pEC50 = 6.3 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
24950242 195419 0 None -12 2 Dog 7.3 pEC50 = 7.3 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 8 3 6 4.4 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1C(=O)O 10.1021/jm800222k
CHEMBL503209 195419 0 None -12 2 Dog 7.3 pEC50 = 7.3 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 8 3 6 4.4 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1C(=O)O 10.1021/jm800222k
45271517 201830 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203998 201830 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549487 201830 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45268128 203101 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203988 203101 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL562315 203101 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10182494 16134 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 451 10 4 4 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)NC1CCCCC1 10.1016/s0960-894x(04)00462-7
CHEMBL111320 16134 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 451 10 4 4 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)NC1CCCCC1 10.1016/s0960-894x(04)00462-7
10301056 20214 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 508 10 3 5 4.3 CC(C)(Cc1ccc(NS(=O)(=O)N2CCC(c3ccccc3)CC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL1193003 20214 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 508 10 3 5 4.3 CC(C)(Cc1ccc(NS(=O)(=O)N2CCC(c3ccccc3)CC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL544336 20214 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 508 10 3 5 4.3 CC(C)(Cc1ccc(NS(=O)(=O)N2CCC(c3ccccc3)CC2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
44472610 144735 0 None -13 4 Dog 7.3 pEC50 = 7.3 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764088 144735 0 None -13 4 Dog 7.3 pEC50 = 7.3 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
10155942 101091 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 369 10 2 7 2.6 COCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL250559 101091 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 369 10 2 7 2.6 COCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
46882028 12530 0 None 100 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 467 11 3 5 4.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1COc1ccccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078495 12530 0 None 100 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 467 11 3 5 4.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1COc1ccccc1 10.1016/j.bmcl.2010.01.130
44298752 203637 0 None 138 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 415 8 1 3 4.5 CCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL56594 203637 0 None 138 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 415 8 1 3 4.5 CCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
10275157 12149 0 None 7 2 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 442 10 5 6 2.2 CNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107012 12149 0 None 7 2 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 442 10 5 6 2.2 CNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
45272431 201888 0 None -51 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204002 201888 0 None -51 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549960 201888 0 None -51 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45273280 202498 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204006 202498 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL557095 202498 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
44127782 203454 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL564556 203454 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44311778 211302 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 347 10 4 6 1.5 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(CO)c2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL72706 211302 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 347 10 4 6 1.5 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(CO)c2)cc1 10.1016/S0960-894X(96)00603-8
24824079 19665 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 441 11 3 5 4.5 O=C(O)COc1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL1188934 19665 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 441 11 3 5 4.5 O=C(O)COc1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL537693 19665 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 441 11 3 5 4.5 O=C(O)COc1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
46881573 15045 0 None 316 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 3 6 2.9 O=C(Cn1ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1092502 15045 0 None 316 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 3 6 2.9 O=C(Cn1ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44396632 74123 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 519 10 4 6 2.7 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)CC(F)(F)F)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188559 74123 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 519 10 4 6 2.7 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)CC(F)(F)F)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
10304786 114770 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 635 15 5 6 5.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL319409 114770 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 635 15 5 6 5.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(02)00607-8
12049923 210450 0 None 181 3 Human 7.3 pEC50 = 7.3 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 608 12 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cc(F)cc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL67404 210450 0 None 181 3 Human 7.3 pEC50 = 7.3 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 608 12 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cc(F)cc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
44589400 201359 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at adrenergic beta-3 receptor in human SK-N-MC cellsAgonist activity at adrenergic beta-3 receptor in human SK-N-MC cells
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
CHEMBL530556 201359 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at adrenergic beta-3 receptor in human SK-N-MC cellsAgonist activity at adrenergic beta-3 receptor in human SK-N-MC cells
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
9907863 122131 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL3349532 122131 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
44335651 115336 0 None 204 3 Human 7.3 pEC50 = 7.3 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 431 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL320228 115336 0 None 204 3 Human 7.3 pEC50 = 7.3 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 431 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00571-x
1028 7079 71 None -4 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
139148732 7079 71 None -4 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
479 7079 71 None -4 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
5816 7079 71 None -4 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
CHEMBL679 7079 71 None -4 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
DB00668 7079 71 None -4 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
24949414 194948 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccnc1Oc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
CHEMBL498704 194948 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccnc1Oc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
9873245 11288 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 590 17 5 7 4.3 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL102194 11288 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 590 17 5 7 4.3 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
44444370 100880 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 507 10 3 6 5.0 Cc1ccc([C@@H](O)CNCCc2ccc(-c3csc(-c4ccccc4)n3)cc2)cc1NS(C)(=O)=O 10.1016/j.bmcl.2007.06.072
CHEMBL249167 100880 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 507 10 3 6 5.0 Cc1ccc([C@@H](O)CNCCc2ccc(-c3csc(-c4ccccc4)n3)cc2)cc1NS(C)(=O)=O 10.1016/j.bmcl.2007.06.072
45269025 202926 0 None -39 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203991 202926 0 None -39 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL561173 202926 0 None -39 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45270391 202233 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 459 11 4 6 3.8 O=C(CC1C=Nc2ccccc21)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552434 202233 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 459 11 4 6 3.8 O=C(CC1C=Nc2ccccc21)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
9907863 122131 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL3349532 122131 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
46881839 13384 0 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 517 11 3 6 5.1 O=C(Cn1nc(-c2ccccc2)cc1-c1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1083216 13384 0 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 517 11 3 6 5.1 O=C(Cn1nc(-c2ccccc2)cc1-c1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
76322043 112684 0 None -3 4 Dog 8.3 pEC50 = 8.3 Functional
Agonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
CHEMBL3128178 112684 0 None -3 4 Dog 8.3 pEC50 = 8.3 Functional
Agonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at dog beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 434 6 3 6 3.6 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2scnc21 10.1021/jm4017224
9849699 80039 16 None -2 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012520 80039 16 None -2 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012521 80039 16 None -2 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012522 80039 16 None -2 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assayAgonist activity at rat adrenergic beta3 receptor expressed in DHB-11 CHO cells assessed as cAMP accumulation after 20 mins by scintillation proximity assay
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
44268482 104875 0 None 199 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 499 12 5 7 2.7 CC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL273428 104875 0 None 199 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 499 12 5 7 2.7 CC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44309272 210657 0 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 611 14 6 8 2.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL68766 210657 0 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 611 14 6 8 2.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(03)00387-1
44331302 215107 0 None 6 3 Human 8.3 pEC50 = 8.3 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 667 12 6 8 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL99219 215107 0 None 6 3 Human 8.3 pEC50 = 8.3 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 667 12 6 8 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44402839 77908 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 609 12 3 7 6.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cc4ccccc4o3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL195508 77908 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 609 12 3 7 6.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cc4ccccc4o3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44307396 210529 0 None 30 3 Human 8.3 pEC50 = 8.3 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 582 12 3 6 3.7 COc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL67886 210529 0 None 30 3 Human 8.3 pEC50 = 8.3 Functional
Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nMEvaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
ChEMBL 582 12 3 6 3.7 COc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
10305108 118220 0 None 77 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 659 17 6 8 4.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL327519 118220 0 None 77 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 659 17 6 8 4.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)CC2)cc1 10.1016/s0960-894x(02)00607-8
44298822 201775 0 None 794 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 460 8 1 3 6.7 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)c1 10.1016/s0960-894x(99)00277-2
CHEMBL54750 201775 0 None 794 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 460 8 1 3 6.7 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)c1 10.1016/s0960-894x(99)00277-2
44336319 13135 0 None 524 2 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 617 12 6 7 3.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
CHEMBL108214 13135 0 None 524 2 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 617 12 6 7 3.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
11556330 169990 0 None 457 3 Human 8.3 pEC50 = 8.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL418308 169990 0 None 457 3 Human 8.3 pEC50 = 8.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44280903 106736 0 None 109 3 Human 8.3 pEC50 = 8.3 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 605 12 3 8 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286437 106736 0 None 109 3 Human 8.3 pEC50 = 8.3 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 605 12 3 8 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
10863093 57101 0 None 3 3 Human 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL157210 57101 0 None 3 3 Human 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
10225563 20981 0 None -12 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1084891 20981 0 None -12 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198889 20981 0 None -12 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
46832232 20987 0 None -39 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1085837 20987 0 None -39 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1198923 20987 0 None -39 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
44298515 202627 0 None 120 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 436 9 1 5 5.1 CCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL55852 202627 0 None 120 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 436 9 1 5 5.1 CCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
24894127 101250 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 518 11 4 7 3.6 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(C)(C)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL251372 101250 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 518 11 4 7 3.6 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(C)(C)C(=O)N2 10.1016/j.bmcl.2007.09.011
44419315 148293 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 519 12 4 8 3.0 CCn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
CHEMBL384560 148293 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 519 12 4 8 3.0 CCn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
44419324 175182 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 533 13 4 8 3.4 CCCn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
CHEMBL434763 175182 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 533 13 4 8 3.4 CCCn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
44268568 31707 0 None 57 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 570 16 6 7 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13459 31707 0 None 57 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 570 16 6 7 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
12017010 169980 0 None 630 3 Human 8.3 pEC50 = 8.3 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 572 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL418234 169980 0 None 630 3 Human 8.3 pEC50 = 8.3 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 572 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
24950059 181649 0 None 169 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL456352 181649 0 None 169 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
12017016 106942 0 None 60 3 Human 8.3 pEC50 = 8.3 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 574 14 3 7 5.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL287947 106942 0 None 60 3 Human 8.3 pEC50 = 8.3 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 574 14 3 7 5.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
9927453 103462 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL26393 103462 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
44268341 29529 0 None 117 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 492 11 4 6 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00169-3
CHEMBL13278 29529 0 None 117 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 492 11 4 6 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00169-3
127042181 143769 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 458 6 2 7 2.1 Cn1nnc([C@@H]2[C@H]3CN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)C[C@H]32)n1 10.1016/j.bmcl.2015.11.030
CHEMBL3745890 143769 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 458 6 2 7 2.1 Cn1nnc([C@@H]2[C@H]3CN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)C[C@H]32)n1 10.1016/j.bmcl.2015.11.030
44419316 91033 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 559 14 4 8 3.8 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL221188 91033 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 559 14 4 8 3.8 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CC3)c12 10.1016/j.bmcl.2006.08.010
44377514 63288 0 None 134 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL163579 63288 0 None 134 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
1960 9632 67 None -1 19 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
439260 9632 67 None -1 19 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
505 9632 67 None -1 19 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
CHEMBL1437 9632 67 None -1 19 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
DB00368 9632 67 None -1 19 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
24823626 104822 0 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1cccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
CHEMBL273098 104822 0 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1cccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
42640122 202954 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL492401 202954 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL561335 202954 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
42640122 202954 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL492401 202954 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL561335 202954 0 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44298769 203886 0 None 79 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 457 12 1 5 6.6 CCCCCCCCc1csc(N(C)c2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL56767 203886 0 None 79 3 Human 8.3 pEC50 = 8.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 457 12 1 5 6.6 CCCCCCCCc1csc(N(C)c2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
10835216 117433 0 None 251 2 Rat 8.3 pEC50 = 8.3 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 406 9 5 5 3.6 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32586 117433 0 None 251 2 Rat 8.3 pEC50 = 8.3 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 406 9 5 5 3.6 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
24950053 194766 0 None 117 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 443 7 3 5 5.1 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)s1 10.1021/jm800222k
CHEMBL497280 194766 0 None 117 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 443 7 3 5 5.1 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)s1 10.1021/jm800222k
10054165 91551 1 None 131 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 14 3 6 5.0 O=C1N(CCCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL22317 91551 1 None 131 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 14 3 6 5.0 O=C1N(CCCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
10054165 91551 1 None 131 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 6 5.0 O=C1N(CCCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22317 91551 1 None 131 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 6 5.0 O=C1N(CCCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
1499 8872 47 None -190 38 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
3779 8872 47 None -190 38 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
536 8872 47 None -190 38 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
CHEMBL434 8872 47 None -190 38 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
DB01064 8872 47 None -190 38 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA methodAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2007.11.060
24950403 194791 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 8 3 4 4.7 O=C(O)COc1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
CHEMBL497453 194791 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 8 3 4 4.7 O=C(O)COc1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1 10.1021/jm800222k
44377316 126840 0 None 173 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 13 3 6 5.0 O=C1N(CCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL350590 126840 0 None 173 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 591 13 3 6 5.0 O=C1N(CCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44402692 140363 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 625 12 3 7 7.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cc4ccccc4s3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL371219 140363 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 625 12 3 7 7.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cc4ccccc4s3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301881 107311 0 None 16218 3 Human 8.2 pEC50 = 8.2 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 612 11 3 8 6.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4s3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL291306 107311 0 None 16218 3 Human 8.2 pEC50 = 8.2 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 612 11 3 8 6.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4s3)cs2)cc1 10.1016/s0960-894x(00)00390-5
9912580 24857 0 None 18 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 470 13 4 6 2.9 O=S(=O)(CCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12674 24857 0 None 18 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 470 13 4 6 2.9 O=S(=O)(CCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
567 7512 16 None -2 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.11.060
9841972 7512 16 None -2 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.11.060
CHEMBL284782 7512 16 None -2 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.11.060
44472610 144735 0 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764088 144735 0 None -1 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
15523860 126949 0 None 851 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 593 15 3 6 5.2 CCCCC(C)(C)CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL351596 126949 0 None 851 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 593 15 3 6 5.2 CCCCC(C)(C)CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
44402822 142815 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 620 17 4 7 5.2 CC(=O)NCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
CHEMBL373188 142815 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 620 17 4 7 5.2 CC(=O)NCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
10302342 116563 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 538 14 5 6 4.5 O=C(NCCCC1CCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL323258 116563 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 538 14 5 6 4.5 O=C(NCCCC1CCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44301886 107856 0 None 316 3 Human 7.3 pEC50 = 7.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 607 16 4 8 4.7 CC(=O)NCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL294849 107856 0 None 316 3 Human 7.3 pEC50 = 7.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 607 16 4 8 4.7 CC(=O)NCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
9893058 73156 0 None -39 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
CHEMBL1814267 73156 0 None -39 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
CHEMBL1851721 73156 0 None -39 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
56943485 119280 0 None -50 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298831 119280 0 None -50 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
42625823 19451 0 None -251 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187371 19451 0 None -251 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL500782 19451 0 None -251 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
44127575 201603 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1cccs1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL539226 201603 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1cccs1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
42625511 19509 0 None -630 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL1187778 19509 0 None -630 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL520313 19509 0 None -630 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
44402689 139942 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 601 16 3 6 7.2 CC/C=C/CC/C=C/c1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
CHEMBL370394 139942 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 601 16 3 6 7.2 CC/C=C/CC/C=C/c1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
44301764 107408 0 None 12 3 Human 7.3 pEC50 = 7.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 564 15 3 7 6.0 CCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL291992 107408 0 None 12 3 Human 7.3 pEC50 = 7.3 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 564 15 3 7 6.0 CCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
44574758 185322 0 None 18 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 394 11 4 5 2.2 O=C(Cc1ncc[nH]1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466879 185322 0 None 18 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 394 11 4 5 2.2 O=C(Cc1ncc[nH]1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
45267257 203461 0 None -41 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203987 203461 0 None -41 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL564648 203461 0 None -41 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
44392559 130092 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 557 11 3 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(N(C)S(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL361577 130092 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 557 11 3 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(N(C)S(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
12049914 210372 0 None 165 3 Human 7.3 pEC50 = 7.3 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL66908 210372 0 None 165 3 Human 7.3 pEC50 = 7.3 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
10666106 121311 0 None 30 2 Rat 7.3 pEC50 = 7.3 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 358 9 4 5 2.2 C[C@H](NCCc1ccc(N(C)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL33360 121311 0 None 30 2 Rat 7.3 pEC50 = 7.3 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 358 9 4 5 2.2 C[C@H](NCCc1ccc(N(C)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
10193354 100938 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2ncco2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL249533 100938 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2ncco2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
49861320 61740 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204003 61740 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1615579 61740 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44127374 203013 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccncc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561693 203013 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccncc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
10746499 121236 0 None 33 3 Human 7.3 pEC50 = 7.3 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccc3C(F)(F)F)cs2)cc1 10.1021/jm000286i
CHEMBL333417 121236 0 None 33 3 Human 7.3 pEC50 = 7.3 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccc3C(F)(F)F)cs2)cc1 10.1021/jm000286i
1499 8872 47 None -190 38 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
3779 8872 47 None -190 38 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
536 8872 47 None -190 38 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
CHEMBL434 8872 47 None -190 38 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
DB01064 8872 47 None -190 38 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
45273280 202498 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204006 202498 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL557095 202498 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
127037832 144830 0 None -147 4 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
CHEMBL3765335 144830 0 None -147 4 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 432 7 3 6 2.8 C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O 10.1021/acs.jmedchem.5b01372
10183401 16070 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 10 3 4 4.1 CN(C1CCCCC1)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL110969 16070 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 465 10 3 4 4.1 CN(C1CCCCC1)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(04)00462-7
44268273 103855 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1Cl 10.1016/s0960-894x(98)00169-3
CHEMBL267306 103855 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1Cl 10.1016/s0960-894x(98)00169-3
44280858 106589 0 None 46 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 577 17 3 8 5.7 CCCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL285458 106589 0 None 46 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 577 17 3 8 5.7 CCCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44574723 185302 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 11 3 5 3.5 O=C(Cc1cccc(Cl)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466726 185302 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 11 3 5 3.5 O=C(Cc1cccc(Cl)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
52941603 24071 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 573 9 2 9 3.8 O=C(c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1)N1CCOCC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257204 24071 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 573 9 2 9 3.8 O=C(c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1)N1CCOCC1 10.1016/j.bmcl.2010.08.039
44309649 211071 0 None 186 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 436 9 3 7 1.6 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL71348 211071 0 None 186 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 436 9 3 7 1.6 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(03)00387-1
10211392 214943 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 629 17 5 7 4.1 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3cccc4c3CC(=O)N4)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL98266 214943 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 629 17 5 7 4.1 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3cccc4c3CC(=O)N4)CC2)cc1 10.1016/s0960-894x(02)00607-8
44298306 108776 0 None 45 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 6 1 3 4.1 CN(CCc1ccccc1)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL301594 108776 0 None 45 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 6 1 3 4.1 CN(CCc1ccccc1)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44298761 201793 0 None 131 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 331 3 2 3 2.2 CNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL54885 201793 0 None 131 3 Human 7.3 pEC50 = 7.3 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 331 3 2 3 2.2 CNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
145984324 172618 0 None 7 3 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 449 11 4 4 4.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=S)Nc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4248727 172618 0 None 7 3 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 449 11 4 4 4.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=S)Nc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
45269866 202073 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448072 202073 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL551389 202073 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45273276 202463 0 None -141 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204005 202463 0 None -141 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL556689 202463 0 None -141 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44127056 202144 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1ccsc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL551892 202144 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1ccsc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
164451 109954 14 None - 1 Human 6.3 pEC50 = 6.3 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.
ChEMBL 361 12 3 6 1.6 O=C(O)COc1ccc(OCCNC[C@H](O)COc2ccccc2)cc1 10.1016/0960-894X(96)00417-9
CHEMBL308150 109954 14 None - 1 Human 6.3 pEC50 = 6.3 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.
ChEMBL 361 12 3 6 1.6 O=C(O)COc1ccc(OCCNC[C@H](O)COc2ccccc2)cc1 10.1016/0960-894X(96)00417-9
44335499 11764 0 None 107 3 Human 7.3 pEC50 = 7.3 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 439 10 3 5 3.9 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104981 11764 0 None 107 3 Human 7.3 pEC50 = 7.3 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 439 10 3 5 3.9 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44303192 210064 0 None 123 3 Human 7.3 pEC50 = 7.3 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 523 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL64697 210064 0 None 123 3 Human 7.3 pEC50 = 7.3 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 523 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00571-x
44579649 193746 0 None 12 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 408 10 3 6 3.4 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL490415 193746 0 None 12 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 408 10 3 6 3.4 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44127481 202931 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)c1 10.1016/j.ejmech.2009.01.022
CHEMBL561211 202931 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)c1 10.1016/j.ejmech.2009.01.022
44311447 210909 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 386 9 4 6 1.9 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c3c2CCC(=O)N3)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL70399 210909 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 386 9 4 6 1.9 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c3c2CCC(=O)N3)cc1 10.1016/S0960-894X(96)00603-8
10292413 101054 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 367 9 2 6 3.6 CC(C)c1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL250352 101054 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 367 9 2 6 3.6 CC(C)c1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
9946573 161532 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 353 9 2 6 3.0 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL400049 161532 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 353 9 2 6 3.0 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
45272431 201888 0 None -51 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204002 201888 0 None -51 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549960 201888 0 None -51 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45270673 202203 0 None -58 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203992 202203 0 None -58 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552253 202203 0 None -58 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
10693556 119121 0 None 2 2 Rat 6.2 pEC50 = 6.2 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 422 9 5 5 2.9 C[C@H](NCCc1ccc(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32939 119121 0 None 2 2 Rat 6.2 pEC50 = 6.2 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 422 9 5 5 2.9 C[C@H](NCCc1ccc(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
10915880 84021 0 None 10 3 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL2079599 84021 0 None 10 3 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
44268358 26198 0 None 52 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 510 11 4 6 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00169-3
CHEMBL12945 26198 0 None 52 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 510 11 4 6 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00169-3
10231394 174595 0 None 190 2 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 562 15 5 7 3.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL430662 174595 0 None 190 2 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 562 15 5 7 3.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
10273469 101029 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 417 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250144 101029 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 417 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
45272430 202223 0 None -36 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204001 202223 0 None -36 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552374 202223 0 None -36 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
46881797 14389 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 517 11 3 6 5.1 O=C(Cn1ncc(-c2ccccc2)c1-c1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1088076 14389 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 517 11 3 6 5.1 O=C(Cn1ncc(-c2ccccc2)c1-c1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
10915880 84021 0 None 10 3 Human 5.2 pEC50 = 5.2 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL2079599 84021 0 None 10 3 Human 5.2 pEC50 = 5.2 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
9912443 194877 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1C(=O)O 10.1021/jm800222k
CHEMBL498145 194877 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1C(=O)O 10.1021/jm800222k
45269373 203115 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(N)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL562395 203115 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 511 11 4 7 3.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(N)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
24895787 193473 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
CHEMBL488431 193473 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
44461486 212142 0 None 741 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 564 15 3 9 3.7 CCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL79806 212142 0 None 741 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 564 15 3 9 3.7 CCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44377771 172326 0 None 70 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 596 10 5 9 3.4 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(=O)(=O)c5ccccc5)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL424167 172326 0 None 70 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 596 10 5 9 3.4 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(=O)(=O)c5ccccc5)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
9828477 68537 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 532 8 5 9 2.4 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(/C=C4\SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL177185 68537 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 532 8 5 9 2.4 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(/C=C4\SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
44386374 137478 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 605 8 4 9 3.7 O=C1CCc2c(OC[C@@H](O)CNC3CCN(c4ccc(/C=C5\SC(N6CCCCC6)=NC5=O)cc4)CC3)ccc(O)c2N1 10.1016/s0960-894x(01)00147-0
CHEMBL368392 137478 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 605 8 4 9 3.7 O=C1CCc2c(OC[C@@H](O)CNC3CCN(c4ccc(/C=C5\SC(N6CCCCC6)=NC5=O)cc4)CC3)ccc(O)c2N1 10.1016/s0960-894x(01)00147-0
44331426 11195 0 None -1 3 Human 8.2 pEC50 = 8.2 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 578 13 7 9 1.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101521 11195 0 None -1 3 Human 8.2 pEC50 = 8.2 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 578 13 7 9 1.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44331346 215168 0 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 638 17 5 8 4.2 CCCCCCCCC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
CHEMBL99599 215168 0 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 638 17 5 8 4.2 CCCCCCCCC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
44307205 210595 0 None 107 3 Human 8.2 pEC50 = 8.2 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 584 17 6 8 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL68408 210595 0 None 107 3 Human 8.2 pEC50 = 8.2 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 584 17 6 8 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
9853471 211633 0 None 177 3 Human 8.2 pEC50 = 8.2 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL75604 211633 0 None 177 3 Human 8.2 pEC50 = 8.2 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
10371216 106523 0 None 162 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285001 106523 0 None 162 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44281395 106706 0 None 416 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 587 13 4 10 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccccc3O)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286231 106706 0 None 416 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 587 13 4 10 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccccc3O)n2)cc1 10.1016/s0960-894x(00)00268-7
44281384 126090 0 None 331 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 601 14 3 10 4.4 COc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL34406 126090 0 None 331 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 601 14 3 10 4.4 COc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44402803 139518 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 601 13 3 6 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(Cc3ccc(F)cc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL369939 139518 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 601 13 3 6 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(Cc3ccc(F)cc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301803 174585 0 None 407 3 Human 8.2 pEC50 = 8.2 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 588 12 3 7 5.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL430594 174585 0 None 407 3 Human 8.2 pEC50 = 8.2 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 588 12 3 7 5.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
9915238 204945 2 None 478 3 Human 8.2 pEC50 = 8.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL57486 204945 2 None 478 3 Human 8.2 pEC50 = 8.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
9933039 169824 0 None -1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
CHEMBL417613 169824 0 None -1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
1960 9632 67 None -1 19 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
439260 9632 67 None -1 19 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
505 9632 67 None -1 19 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
CHEMBL1437 9632 67 None -1 19 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
DB00368 9632 67 None -1 19 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assayAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2007.11.060
9933039 169824 0 None -1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00170-x
CHEMBL417613 169824 0 None -1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00170-x
44457929 91552 0 None 91 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 593 17 3 10 3.9 CCCCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
CHEMBL22318 91552 0 None 91 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 593 17 3 10 3.9 CCCCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
9915238 204945 2 None 478 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00277-2
CHEMBL57486 204945 2 None 478 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00277-2
10841426 123650 0 None 316 3 Human 8.2 pEC50 = 8.2 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 610 11 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc(F)c(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL338216 123650 0 None 316 3 Human 8.2 pEC50 = 8.2 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 610 11 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc(F)c(F)c(F)c3)cs2)cc1 10.1021/jm000286i
9915238 204945 2 None 478 3 Human 8.2 pEC50 = 8.2 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL57486 204945 2 None 478 3 Human 8.2 pEC50 = 8.2 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(00)00422-4
9984028 126504 0 None 794 3 Human 8.2 pEC50 = 8.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2cccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1021/jm0101500
CHEMBL347582 126504 0 None 794 3 Human 8.2 pEC50 = 8.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2cccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1021/jm0101500
9984028 126504 0 None 794 3 Human 8.2 pEC50 = 8.2 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2cccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1021/jm0509445
CHEMBL347582 126504 0 None 794 3 Human 8.2 pEC50 = 8.2 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2cccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1021/jm0509445
44441228 174551 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2nc(C(=O)O)cs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL430390 174551 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2nc(C(=O)O)cs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
90645344 119233 0 None -19 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 119233 0 None -19 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
12049919 209878 0 None 58 3 Human 8.2 pEC50 = 8.2 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63963 209878 0 None 58 3 Human 8.2 pEC50 = 8.2 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
44307148 210122 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 586 12 3 9 3.7 O=C(c1ccc(F)cc1)c1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00422-4
CHEMBL64991 210122 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 586 12 3 9 3.7 O=C(c1ccc(F)cc1)c1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00422-4
44579940 198671 0 None 37 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc(C(=O)O)c1 10.1016/j.bmcl.2008.08.009
CHEMBL519985 198671 0 None 37 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc(C(=O)O)c1 10.1016/j.bmcl.2008.08.009
24894127 101250 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta-3 adrenergic receptorAgonist activity at rat beta-3 adrenergic receptor
ChEMBL 518 11 4 7 3.6 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(C)(C)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL251372 101250 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta-3 adrenergic receptorAgonist activity at rat beta-3 adrenergic receptor
ChEMBL 518 11 4 7 3.6 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C(C)(C)C(=O)N2 10.1016/j.bmcl.2007.09.011
11152564 106791 0 None 4 2 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL286818 106791 0 None 4 2 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
44392577 129320 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 455 10 4 6 3.2 CC#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL360133 129320 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 455 10 4 6 3.2 CC#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44444173 100756 0 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 516 11 4 7 3.3 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL248547 100756 0 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 516 11 4 7 3.3 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
44579941 190890 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 3 5 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1N1CCCC1=O 10.1016/j.bmcl.2008.08.009
CHEMBL482627 190890 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 3 5 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1N1CCCC1=O 10.1016/j.bmcl.2008.08.009
44268569 104970 0 None 43 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 598 17 5 7 4.5 CCCCCCNC(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL274143 104970 0 None 43 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 598 17 5 7 4.5 CCCCCCNC(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
24822310 104517 0 None 41 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL271576 104517 0 None 41 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
24822310 104517 0 None 41 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2008.08.009
CHEMBL271576 104517 0 None 41 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2008.08.009
24822310 104517 0 None 41 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm800222k
CHEMBL271576 104517 0 None 41 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm800222k
44396671 73493 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 587 10 4 7 4.6 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL185636 73493 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 587 10 4 7 4.6 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44419316 91033 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 559 14 4 8 3.8 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL221188 91033 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at rat beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 559 14 4 8 3.8 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CC3)c12 10.1016/j.bmcl.2006.08.010
44268470 31642 0 None 33 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 527 14 5 7 3.5 CCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13453 31642 0 None 33 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity towards human Beta-3 adrenergic receptorAgonist activity towards human Beta-3 adrenergic receptor
ChEMBL 527 14 5 7 3.5 CCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
46881617 14715 0 None 1230 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 397 9 4 7 2.2 Nc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
CHEMBL1090425 14715 0 None 1230 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 397 9 4 7 2.2 Nc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
46882029 12531 0 None 87 2 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCn2cccc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078496 12531 0 None 87 2 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCn2cccc2)c1 10.1016/j.bmcl.2010.01.130
44298728 201562 0 None 5248 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 401 8 2 3 4.1 CCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL53842 201562 0 None 5248 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 401 8 2 3 4.1 CCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
10627736 123774 0 None 141 3 Human 8.2 pEC50 = 8.2 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(C(F)(F)F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL338794 123774 0 None 141 3 Human 8.2 pEC50 = 8.2 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(C(F)(F)F)c3)cs2)cc1 10.1021/jm000286i
44268295 105320 0 None 8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 408 12 4 6 2.1 CCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL276480 105320 0 None 8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 408 12 4 6 2.1 CCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44579964 193898 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1016/j.bmcl.2008.08.009
CHEMBL491634 193898 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 411 9 3 4 4.7 O=C(O)c1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1016/j.bmcl.2008.08.009
44461716 212091 0 None 33 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 605 17 3 8 5.4 CCCCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL79363 212091 0 None 33 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 605 17 3 8 5.4 CCCCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
10301101 109737 0 None 1659 2 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 509 9 3 6 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL306423 109737 0 None 1659 2 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 509 9 3 6 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
9908924 148433 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL38538 148433 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
10281165 11185 0 None 16 2 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 560 11 5 7 3.3 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)NC1CCCCC1 10.1016/s0960-894x(02)00607-8
CHEMBL101485 11185 0 None 16 2 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 560 11 5 7 3.3 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)NC1CCCCC1 10.1016/s0960-894x(02)00607-8
10553602 133930 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 506 10 6 8 0.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL36568 133930 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 506 10 6 8 0.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
44268214 25341 0 None -39 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 331 10 3 5 2.4 COc1ccc(CCCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12762 25341 0 None -39 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 331 10 3 5 2.4 COc1ccc(CCCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44268264 105008 0 None -120 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL274361 105008 0 None -120 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
45271523 201907 0 None -61 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204000 201907 0 None -61 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550096 201907 0 None -61 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
9962058 211561 0 None 165 3 Human 6.2 pEC50 = 6.2 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL74860 211561 0 None 165 3 Human 6.2 pEC50 = 6.2 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)cc2)cc1 10.1016/s0960-894x(00)00459-5
44268267 25211 0 None -199 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12719 25211 0 None -199 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44444393 173194 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 353 8 2 6 3.1 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)c(C)o1 10.1016/j.bmcl.2007.06.072
CHEMBL427711 173194 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 353 8 2 6 3.1 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)c(C)o1 10.1016/j.bmcl.2007.06.072
24824227 165131 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 11 3 5 3.9 O=C(O)COc1ccc(C(=O)c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL408958 165131 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 11 3 5 3.9 O=C(O)COc1ccc(C(=O)c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
10573759 106455 0 None 20 2 Rat 7.2 pEC50 = 7.2 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL284520 106455 0 None 20 2 Rat 7.2 pEC50 = 7.2 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
45272417 202220 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448074 202220 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552368 202220 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45273281 202517 0 None -12 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448075 202517 0 None -12 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL557295 202517 0 None -12 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10981769 84007 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL2079543 84007 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
44287268 165796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 441 11 3 5 4.5 CC(C)OP(=O)(O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
CHEMBL40966 165796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 441 11 3 5 4.5 CC(C)OP(=O)(O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
44472610 144735 0 None -234 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764088 144735 0 None -234 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 418 7 3 6 2.3 O=C(Cn1ncccc1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
10981769 84007 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL2079543 84007 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 379 9 4 5 2.8 C[C@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
10296855 15256 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 437 9 3 4 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)N1CCCCC1 10.1016/s0960-894x(04)00462-7
CHEMBL109397 15256 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 437 9 3 4 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)N1CCCCC1 10.1016/s0960-894x(04)00462-7
44268365 105345 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 406 10 4 5 3.2 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
CHEMBL276659 105345 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 406 10 4 5 3.2 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
50994950 143880 0 None 173 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 450 7 2 5 3.5 CCOC(=O)C1CCN(C(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)CC1 10.1016/j.bmcl.2015.11.030
CHEMBL3747487 143880 0 None 173 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 450 7 2 5 3.5 CCOC(=O)C1CCN(C(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)CC1 10.1016/j.bmcl.2015.11.030
11091850 54005 0 None -63 3 Human 7.2 pEC50 = 7.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL154370 54005 0 None -63 3 Human 7.2 pEC50 = 7.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
11661536 82751 0 None 50 3 Human 7.2 pEC50 = 7.2 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cncc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
CHEMBL205389 82751 0 None 50 3 Human 7.2 pEC50 = 7.2 Functional
Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cncc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
56678847 73151 0 None -99 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814274 73151 0 None -99 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851691 73151 0 None -99 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
53357712 73181 0 None -79 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814271 73181 0 None -79 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851848 73181 0 None -79 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
11169365 119289 0 None -223 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298986 119289 0 None -223 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
46833103 14185 0 None -7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(O)cc2)ccc1O 10.1021/jm100326d
CHEMBL1086535 14185 0 None -7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(O)cc2)ccc1O 10.1021/jm100326d
44517696 202550 0 None -17 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204007 202550 0 None -17 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL557705 202550 0 None -17 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
9821129 211219 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
ChEMBL 378 12 3 6 2.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL72169 211219 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
ChEMBL 378 12 3 6 2.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
42625897 19248 0 None -501 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
CHEMBL1186265 19248 0 None -501 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
CHEMBL456485 19248 0 None -501 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
42625821 19316 0 None -630 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186678 19316 0 None -630 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL474393 19316 0 None -630 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
443372 17006 26 None -7585 9 Rat 4.2 pEC50 = 4.2 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL1160723 17006 26 None -7585 9 Rat 4.2 pEC50 = 4.2 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL2062275 17006 26 None -7585 9 Rat 4.2 pEC50 = 4.2 Functional
Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
45381933 129317 0 None 12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601308 129317 0 None 12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
46881698 13940 0 None 21 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 458 10 3 5 2.9 O=C(CN1CC(c2ccccc2)CC1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1085444 13940 0 None 21 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 458 10 3 5 2.9 O=C(CN1CC(c2ccccc2)CC1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44281343 117146 0 None 123 3 Human 7.2 pEC50 = 7.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 639 14 3 13 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(C4N=NN=N4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL32418 117146 0 None 123 3 Human 7.2 pEC50 = 7.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 639 14 3 13 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(C4N=NN=N4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
10112744 161434 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccncc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL399522 161434 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccncc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
45271523 201907 0 None -61 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204000 201907 0 None -61 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550096 201907 0 None -61 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
44127677 202184 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1ccc2ccccc2n1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552089 202184 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1ccc2ccccc2n1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44281074 121907 0 None 181 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 14 3 9 3.7 CCC(=O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33438 121907 0 None 181 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 549 14 3 9 3.7 CCC(=O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
45280021 129316 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 444 10 4 6 2.9 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CCC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601307 129316 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 444 10 4 6 2.9 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CCC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
10232593 12169 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 609 17 6 7 4.8 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107129 12169 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 609 17 6 7 4.8 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)cc2)CC1 10.1016/s0960-894x(01)00645-x
10601234 118784 0 None 23 3 Human 7.2 pEC50 = 7.2 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 493 11 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(COCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32888 118784 0 None 23 3 Human 7.2 pEC50 = 7.2 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 493 11 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(COCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
9831168 211481 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL74085 211481 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
44377804 176000 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 552 9 4 8 2.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1Cl 10.1016/s0960-894x(01)00063-4
CHEMBL440924 176000 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 552 9 4 8 2.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1Cl 10.1016/s0960-894x(01)00063-4
10160281 11009 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 437 12 3 4 4.9 CCCCCCN1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
CHEMBL100414 11009 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 437 12 3 4 4.9 CCCCCCN1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
44335663 11562 0 None 12 3 Human 7.2 pEC50 = 7.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 560 13 4 7 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1)OCCc1ccccc1 10.1016/s0960-894x(98)00571-x
CHEMBL104076 11562 0 None 12 3 Human 7.2 pEC50 = 7.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 560 13 4 7 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1)OCCc1ccccc1 10.1016/s0960-894x(98)00571-x
44335588 12045 0 None 131 3 Human 7.2 pEC50 = 7.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 496 13 4 6 3.9 CCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL106487 12045 0 None 131 3 Human 7.2 pEC50 = 7.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 496 13 4 6 3.9 CCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44377665 175112 0 None 741 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 567 15 3 7 3.4 COCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL434284 175112 0 None 741 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 567 15 3 7 3.4 COCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
46881902 14618 0 None 77 2 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 430 9 3 5 3.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1N1CCCC1 10.1016/j.bmcl.2010.01.130
CHEMBL1089735 14618 0 None 77 2 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 430 9 3 5 3.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1N1CCCC1 10.1016/j.bmcl.2010.01.130
44335618 11559 0 None 29 3 Human 7.2 pEC50 = 7.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 497 12 5 6 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104061 11559 0 None 29 3 Human 7.2 pEC50 = 7.2 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 497 12 5 6 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
567 7512 16 None -2 7 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
9841972 7512 16 None -2 7 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
CHEMBL284782 7512 16 None -2 7 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
567 7512 16 None -2 7 Human 6.2 pEC50 = 6.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
9841972 7512 16 None -2 7 Human 6.2 pEC50 = 6.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
CHEMBL284782 7512 16 None -2 7 Human 6.2 pEC50 = 6.2 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
44574868 185353 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nccn1Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467103 185353 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nccn1Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
11163954 101439 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptorAgonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptor
ChEMBL 314 6 3 2 3.7 OC(CNCCc1c[nH]c2ccccc12)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25254 101439 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptorAgonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptor
ChEMBL 314 6 3 2 3.7 OC(CNCCc1c[nH]c2ccccc12)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
46881614 15135 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 366 9 3 7 1.2 O=C(Cn1cncn1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1093086 15135 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 366 9 3 7 1.2 O=C(Cn1cncn1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
10225274 20455 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 440 10 4 5 3.5 CC(C)(Cc1ccc(NS(=O)(=O)Nc2ccccc2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL1194766 20455 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 440 10 4 5 3.5 CC(C)(Cc1ccc(NS(=O)(=O)Nc2ccccc2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
CHEMBL553279 20455 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 440 10 4 5 3.5 CC(C)(Cc1ccc(NS(=O)(=O)Nc2ccccc2)cc1)NC[C@H](O)c1cccnc1 10.1016/s0960-894x(04)00462-7
44312949 210543 0 None 42 3 Human 8.2 pEC50 = 8.2 Functional
Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nMCompound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
ChEMBL 602 11 6 6 6.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(CC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL67998 210543 0 None 42 3 Human 8.2 pEC50 = 8.2 Functional
Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nMCompound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
ChEMBL 602 11 6 6 6.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(CC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
44307343 210382 0 None 74 3 Human 8.2 pEC50 = 8.2 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 457 12 3 7 2.5 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL66964 210382 0 None 74 3 Human 8.2 pEC50 = 8.2 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 457 12 3 7 2.5 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44298695 107712 0 None 141 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 414 10 1 3 5.1 CCCCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL294008 107712 0 None 141 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 414 10 1 3 5.1 CCCCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44281372 106894 0 None 354 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 621 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL287562 106894 0 None 354 3 Human 8.2 pEC50 = 8.2 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 621 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44419332 148538 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 505 11 4 8 2.5 Cn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
CHEMBL386016 148538 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 505 11 4 8 2.5 Cn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
24949262 194851 1 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL497847 194851 1 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
52949934 24420 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 398 7 2 7 3.0 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258372 24420 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 398 7 2 7 3.0 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
10100 10759 30 None -1 4 Rhesus macaque 8.2 pEC50 = 8.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None -1 4 Rhesus macaque 8.2 pEC50 = 8.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None -1 4 Rhesus macaque 8.2 pEC50 = 8.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None -1 4 Rhesus macaque 8.2 pEC50 = 8.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None -1 4 Rhesus macaque 8.2 pEC50 = 8.2 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44402731 78209 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 605 12 3 6 6.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL196081 78209 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 605 12 3 6 6.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
11758172 107711 0 None 147 3 Human 8.2 pEC50 = 8.2 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL293994 107711 0 None 147 3 Human 8.2 pEC50 = 8.2 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
11758172 107711 0 None 147 3 Human 8.2 pEC50 = 8.2 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL293994 107711 0 None 147 3 Human 8.2 pEC50 = 8.2 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44580011 193579 0 None 52 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL489200 193579 0 None 52 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
10438390 210181 0 None 138 3 Human 8.1 pEC50 = 8.1 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL65513 210181 0 None 138 3 Human 8.1 pEC50 = 8.1 Functional
Tested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptorTested in vitro for its ability to stimulate increase in cAMP in CHO cells expressing the cloned human beta-3 adrenergic receptor
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
10809699 119115 0 None 8 2 Rat 8.1 pEC50 = 8.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32933 119115 0 None 8 2 Rat 8.1 pEC50 = 8.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44402693 140364 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cnc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL371220 140364 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3cnc4ccccc4c3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301979 107639 0 None 2630 3 Human 8.1 pEC50 = 8.1 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cnc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL293577 107639 0 None 2630 3 Human 8.1 pEC50 = 8.1 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cnc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44560739 180591 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 5 4.1 CC(C)Oc1cc(-c2ccc(C[C@H](CO)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453835 180591 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 5 4.1 CC(C)Oc1cc(-c2ccc(C[C@H](CO)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11611195 20223 0 None 70 3 Human 8.1 pEC50 = 8.1 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL1193081 20223 0 None 70 3 Human 8.1 pEC50 = 8.1 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL544427 20223 0 None 70 3 Human 8.1 pEC50 = 8.1 Functional
Concentration required to effect a 50% relaxation of ferret detrusor basal toneConcentration required to effect a 50% relaxation of ferret detrusor basal tone
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
11611195 20223 0 None 70 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL1193081 20223 0 None 70 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL544427 20223 0 None 70 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
24822469 104553 0 None 26 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 401 8 3 4 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)s1 10.1021/jm701324c
CHEMBL271765 104553 0 None 26 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 401 8 3 4 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)s1 10.1021/jm701324c
44396730 73593 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 547 12 4 6 5.5 O=S(=O)(Nc1cccc([C@@H](O)CNCCc2c[nH]c3c(OCc4ccccc4)cccc23)c1)c1cccs1 10.1016/j.bmcl.2004.09.054
CHEMBL186059 73593 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 547 12 4 6 5.5 O=S(=O)(Nc1cccc([C@@H](O)CNCCc2c[nH]c3c(OCc4ccccc4)cccc23)c1)c1cccs1 10.1016/j.bmcl.2004.09.054
10651078 24714 0 None 99 3 Human 8.1 pEC50 = 8.1 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(F)c3F)cs2)cc1 10.1021/jm000286i
CHEMBL125963 24714 0 None 99 3 Human 8.1 pEC50 = 8.1 Functional
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptorIn vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(F)c3F)cs2)cc1 10.1021/jm000286i
145982668 172693 0 None 15 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 418 11 3 4 4.1 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4250215 172693 0 None 15 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 418 11 3 4 4.1 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
24937390 24387 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 8 3 8 4.4 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258259 24387 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 490 8 3 8 4.4 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
44303198 209937 0 None 3 3 Human 8.1 pEC50 = 8.1 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 568 11 4 7 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL64201 209937 0 None 3 3 Human 8.1 pEC50 = 8.1 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 568 11 4 7 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
145984792 172508 0 None 776 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 461 12 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)c3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4246134 172508 0 None 776 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 461 12 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)c3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
3038500 16112 12 None -2 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 16112 12 None -2 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serumAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
9801145 100197 0 None 316 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 9 4 5 4.0 O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245874 100197 0 None 316 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 9 4 5 4.0 O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
90645347 119290 0 None -39 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 119290 0 None -39 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
10238776 73250 0 None -10 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835853 73250 0 None -10 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852214 73250 0 None -10 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
46832798 20975 0 None -19 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1084648 20975 0 None -19 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1198879 20975 0 None -19 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
12114484 109710 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 536 8 4 8 3.4 O=S(=O)(c1ccc2oc3ccccc3c2c1)N1CCC(NC[C@H](O)COc2cccc3[nH]c(O)nc23)CC1 10.1016/s0960-894x(03)00387-1
CHEMBL306233 109710 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 536 8 4 8 3.4 O=S(=O)(c1ccc2oc3ccccc3c2c1)N1CCC(NC[C@H](O)COc2cccc3[nH]c(O)nc23)CC1 10.1016/s0960-894x(03)00387-1
11236495 106651 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptorAgonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptor
ChEMBL 342 6 3 2 4.5 CC(C)(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL285899 106651 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptorAgonistic activity against human Beta-3 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing Beta-3 adrenergic receptor
ChEMBL 342 6 3 2 4.5 CC(C)(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
10301445 11062 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist activity by increase in cAMP levels in chinese hamster ovary cells (CHO) cells stimulated by human Beta-3 Adrenoceptor was determinedIn vitro agonist activity by increase in cAMP levels in chinese hamster ovary cells (CHO) cells stimulated by human Beta-3 Adrenoceptor was determined
ChEMBL 516 9 5 5 4.3 O=C(O)c1cccc(NC(=O)N2CCC(CNC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)c1 10.1016/s0960-894x(02)00607-8
CHEMBL100724 11062 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist activity by increase in cAMP levels in chinese hamster ovary cells (CHO) cells stimulated by human Beta-3 Adrenoceptor was determinedIn vitro agonist activity by increase in cAMP levels in chinese hamster ovary cells (CHO) cells stimulated by human Beta-3 Adrenoceptor was determined
ChEMBL 516 9 5 5 4.3 O=C(O)c1cccc(NC(=O)N2CCC(CNC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)c1 10.1016/s0960-894x(02)00607-8
45270680 201817 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203993 201817 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549421 201817 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
44574867 185352 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 562 13 3 6 4.4 O=C(Cc1nccn1Cc1ccc(Br)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467102 185352 0 None 2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 562 13 3 6 4.4 O=C(Cc1nccn1Cc1ccc(Br)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
122184771 129298 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601202 129298 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
46845698 12554 0 None 165 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 444 9 3 5 4.1 Cc1ccc(N2CCCC2)c(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078696 12554 0 None 165 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 444 9 3 5 4.1 Cc1ccc(N2CCCC2)c(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/j.bmcl.2010.01.130
44307064 210114 0 None 5 3 Human 7.1 pEC50 = 7.1 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 461 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64936 210114 0 None 5 3 Human 7.1 pEC50 = 7.1 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 461 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00381-3
9933039 169824 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL417613 169824 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
44574827 185411 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 518 13 3 6 4.3 O=C(Cc1nccn1Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467502 185411 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 518 13 3 6 4.3 O=C(Cc1nccn1Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
46881650 13632 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 396 9 3 6 2.9 Cc1csc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
CHEMBL1084136 13632 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 396 9 3 6 2.9 Cc1csc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.01.130
44392223 72450 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 439 9 5 4 4.2 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183433 72450 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 439 9 5 4 4.2 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2004.11.001
44127050 203452 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccccc1Cl)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL564544 203452 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccccc1Cl)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44281073 125984 0 None 316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 551 14 4 9 3.5 CCC(O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL34328 125984 0 None 316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 551 14 4 9 3.5 CCC(O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
127041869 143840 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 448 7 2 5 3.0 CCOC(=O)[C@H]1[C@H]2CN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)C[C@H]21 10.1016/j.bmcl.2015.11.030
CHEMBL3746885 143840 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 448 7 2 5 3.0 CCOC(=O)[C@H]1[C@H]2CN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)C[C@H]21 10.1016/j.bmcl.2015.11.030
44385716 66387 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 520 8 2 7 4.1 O=C1N=C(N2CCCCC2)S/C1=C\c1ccc(N2CCC(NC[C@H](O)COc3ccccc3)CC2)cc1 10.1016/s0960-894x(01)00147-0
CHEMBL171963 66387 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 520 8 2 7 4.1 O=C1N=C(N2CCCCC2)S/C1=C\c1ccc(N2CCC(NC[C@H](O)COc3ccccc3)CC2)cc1 10.1016/s0960-894x(01)00147-0
44286965 167188 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 349 9 3 4 3.0 C[C@H](Cc1ccc(OCCO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL41113 167188 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranesEffective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
ChEMBL 349 9 3 4 3.0 C[C@H](Cc1ccc(OCCO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
46845699 12576 0 None 208 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 444 9 3 5 4.1 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c(N2CCCC2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078876 12576 0 None 208 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 444 9 3 5 4.1 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c(N2CCCC2)c1 10.1016/j.bmcl.2010.01.130
44285692 144005 0 None 398 3 Human 7.1 pEC50 = 7.1 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 478 10 3 7 3.7 Cc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)co1 10.1016/s0960-894x(00)00277-8
CHEMBL37512 144005 0 None 398 3 Human 7.1 pEC50 = 7.1 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 478 10 3 7 3.7 Cc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)co1 10.1016/s0960-894x(00)00277-8
46881935 13938 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 428 9 3 7 2.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-n1nccn1 10.1016/j.bmcl.2010.01.130
CHEMBL1085441 13938 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 428 9 3 7 2.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-n1nccn1 10.1016/j.bmcl.2010.01.130
76318363 112692 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 391 7 3 6 2.3 O=C(Cn1cccn1)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
CHEMBL3128186 112692 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 391 7 3 6 2.3 O=C(Cn1cccn1)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1 10.1021/jm4017224
45270697 201949 0 None -44 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203995 201949 0 None -44 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550444 201949 0 None -44 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44335572 11945 0 None 64 3 Human 7.1 pEC50 = 7.1 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 475 9 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL105968 11945 0 None 64 3 Human 7.1 pEC50 = 7.1 Functional
Agonism against Beta-3 adrenergic receptorAgonism against Beta-3 adrenergic receptor
ChEMBL 475 9 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00571-x
9933039 169824 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL417613 169824 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
9933039 169824 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL417613 169824 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
9896742 211723 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 618 12 6 7 6.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(OCC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL76403 211723 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 618 12 6 7 6.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(OCC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
52943919 24493 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 500 10 2 7 5.1 C=CCc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258597 24493 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 500 10 2 7 5.1 C=CCc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
44281467 126144 0 None 25 3 Human 7.1 pEC50 = 7.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 648 14 4 10 3.8 CS(=O)(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL34441 126144 0 None 25 3 Human 7.1 pEC50 = 7.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 648 14 4 10 3.8 CS(=O)(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
56672116 73139 0 None -316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814276 73139 0 None -316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851624 73139 0 None -316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
46832509 20984 0 None -316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085399 20984 0 None -316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198908 20984 0 None -316 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
44311757 109781 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 335 9 3 5 2.1 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(F)c2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL306838 109781 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 335 9 3 5 2.1 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(F)c2)cc1 10.1016/S0960-894X(96)00603-8
11002571 54873 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 348 8 4 4 3.2 C[C@H](CNc1ccc(C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL155092 54873 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 348 8 4 4 3.2 C[C@H](CNc1ccc(C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
10184665 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
4799 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
7353 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
CHEMBL1198857 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
DB09082 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
42625515 19502 0 None -1258 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187711 19502 0 None -1258 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL516056 19502 0 None -1258 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
10184665 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
4799 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
7353 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
CHEMBL1198857 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
DB09082 10763 51 None -40 10 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
10204992 20576 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 462 9 3 6 2.5 C[C@H]1CN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)C[C@@H](C)O1 10.1016/s0960-894x(04)00462-7
CHEMBL1195606 20576 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 462 9 3 6 2.5 C[C@H]1CN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)C[C@@H](C)O1 10.1016/s0960-894x(04)00462-7
CHEMBL554963 20576 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 462 9 3 6 2.5 C[C@H]1CN(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)c3cccnc3)cc2)C[C@@H](C)O1 10.1016/s0960-894x(04)00462-7
46881652 13634 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 442 10 4 6 2.9 O=C(Cc1nnc(-c2ccccc2)[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084138 13634 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 442 10 4 6 2.9 O=C(Cc1nnc(-c2ccccc2)[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
10187201 11953 0 None 77 2 Human 8.1 pEC50 = 8.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 540 17 5 6 4.9 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL106022 11953 0 None 77 2 Human 8.1 pEC50 = 8.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 540 17 5 6 4.9 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10008017 106648 10 None 7 3 Human 8.1 pEC50 = 8.1 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 562 12 6 8 2.3 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
CHEMBL285881 106648 10 None 7 3 Human 8.1 pEC50 = 8.1 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 562 12 6 8 2.3 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
44281371 106896 0 None 125 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 655 14 3 10 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL287567 106896 0 None 125 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 655 14 3 10 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
15483883 107008 0 None 501 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL288550 107008 0 None 501 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44281219 118791 0 None 251 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 588 12 4 9 4.0 NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL32891 118791 0 None 251 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 588 12 4 9 4.0 NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
44281470 120351 0 None 316 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 589 12 4 9 4.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(C(O)c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33224 120351 0 None 316 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 589 12 4 9 4.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(C(O)c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
10054896 120916 0 None 162 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33292 120916 0 None 162 3 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptorStimulation of cAMP levels in CHO cells expressing the recombinant human beta-3 adrenergic receptor
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
24895196 185644 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 4 5 4.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(N)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL469685 185644 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 4 5 4.3 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(N)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44298290 174985 0 None 93 3 Human 8.1 pEC50 = 8.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 371 4 1 5 3.9 Cc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL433454 174985 0 None 93 3 Human 8.1 pEC50 = 8.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 371 4 1 5 3.9 Cc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
44444176 100798 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 558 11 4 7 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CCCCC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL248751 100798 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 558 11 4 7 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CCCCC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
53326197 65434 0 None 28 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684584 65434 0 None 28 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
52944986 24385 0 None 26 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
CHEMBL1258257 24385 0 None 26 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
44392240 71093 0 None 6 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 401 12 5 5 2.2 CCCNC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL181115 71093 0 None 6 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
ChEMBL 401 12 5 5 2.2 CCCNC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44396623 73819 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccc(N)cc4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL187131 73819 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccc(N)cc4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
567 7512 16 None 2 7 Rat 8.1 pEC50 = 8.1 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
9841972 7512 16 None 2 7 Rat 8.1 pEC50 = 8.1 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
CHEMBL284782 7512 16 None 2 7 Rat 8.1 pEC50 = 8.1 Functional
In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.In vitro beta-adrenergic activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
145983886 172720 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 474 11 5 5 4.4 COc1ccccc1NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4250942 172720 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 474 11 5 5 4.4 COc1ccccc1NC(=O)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
44580039 193729 0 None 15 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O)c1ccccc1 10.1016/j.bmcl.2008.08.009
CHEMBL490222 193729 0 None 15 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O)c1ccccc1 10.1016/j.bmcl.2008.08.009
145982607 172499 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 432 12 3 4 4.0 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4245968 172499 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta3 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 432 12 3 4 4.0 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
24822304 104640 0 None -6 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 412 9 3 5 4.1 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
CHEMBL272234 104640 0 None -6 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 412 9 3 5 4.1 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
76332892 112691 0 None 281 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 528 7 3 6 5.4 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
CHEMBL3128185 112691 0 None 281 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
ChEMBL 528 7 3 6 5.4 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
46881530 14095 0 None 691 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 4 5 3.0 O=C(Cc1nc2ccccc2[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1086149 14095 0 None 691 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 415 9 4 5 3.0 O=C(Cc1nc2ccccc2[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
135995977 69854 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 547 8 6 10 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NO)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
136727661 69854 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 547 8 6 10 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NO)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL178848 69854 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 547 8 6 10 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NO)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
10142284 11661 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 510 11 5 6 3.9 O=C(NC1CCCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL104481 11661 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 510 11 5 6 3.9 O=C(NC1CCCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
9958539 109882 0 None -104 3 Human 6.1 pEC50 = 6.1 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
CHEMBL307647 109882 0 None -104 3 Human 6.1 pEC50 = 6.1 Functional
Inhibitory activity against human beta-3 adrenergic receptor (AR)Inhibitory activity against human beta-3 adrenergic receptor (AR)
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
53326839 65431 0 None 26 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684581 65431 0 None 26 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
44461717 112457 0 None 24 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 577 15 3 8 4.6 CCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL312546 112457 0 None 24 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 577 15 3 8 4.6 CCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
11799609 121576 0 None 31 2 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 500 9 5 5 3.7 C[C@H](NCCc1cc(Br)c(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL33399 121576 0 None 31 2 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 500 9 5 5 3.7 C[C@H](NCCc1cc(Br)c(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44517694 201950 0 None -17 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203996 201950 0 None -17 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL550445 201950 0 None -17 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
10672048 127890 0 None 2 2 Rat 6.1 pEC50 = 6.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 470 9 5 5 2.7 C[C@H](NCCc1ccc(NCC(=O)O)c(I)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL35738 127890 0 None 2 2 Rat 6.1 pEC50 = 6.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 470 9 5 5 2.7 C[C@H](NCCc1ccc(NCC(=O)O)c(I)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
44311101 108897 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 333 9 4 6 1.7 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(O)c2)cc1 10.1016/S0960-894X(96)00603-8
CHEMBL302370 108897 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cellsAgonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
ChEMBL 333 9 4 6 1.7 COc1ccc(CCNC[C@@H](O)COc2ccc(O)c(O)c2)cc1 10.1016/S0960-894X(96)00603-8
44127679 202241 0 None 37 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 422 11 4 7 1.9 O=C(Cc1cnccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552497 202241 0 None 37 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 422 11 4 7 1.9 O=C(Cc1cnccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44281611 107139 0 None -2 2 Rat 6.1 pEC50 = 6.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 402 11 5 6 1.6 C[C@H](NCCc1ccc(N(CC(=O)O)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL289670 107139 0 None -2 2 Rat 6.1 pEC50 = 6.1 Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 402 11 5 6 1.6 C[C@H](NCCc1ccc(N(CC(=O)O)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
24823468 165130 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 457 11 3 5 4.8 O=C(O)COc1ccc(Sc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL408957 165130 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 457 11 3 5 4.8 O=C(O)COc1ccc(Sc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
44377677 63654 0 None 23 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 495 10 3 6 2.6 CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL164401 63654 0 None 23 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 495 10 3 6 2.6 CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
44307007 107555 0 None 4 3 Human 7.1 pEC50 = 7.1 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 469 12 3 6 3.6 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL292947 107555 0 None 4 3 Human 7.1 pEC50 = 7.1 Functional
Evaluated for its agonist activity against human Beta-3 adrenergic receptorEvaluated for its agonist activity against human Beta-3 adrenergic receptor
ChEMBL 469 12 3 6 3.6 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
10144004 210878 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 551 12 3 6 4.7 CCCCOc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL70230 210878 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 551 12 3 6 4.7 CCCCOc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
44309322 211044 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 504 8 4 10 1.5 O=S(=O)(c1cccc2nsnc12)N1CCC(NC[C@H](O)COc2cccc3[nH]c(O)nc23)CC1 10.1016/s0960-894x(03)00387-1
CHEMBL71192 211044 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 504 8 4 10 1.5 O=S(=O)(c1cccc2nsnc12)N1CCC(NC[C@H](O)COc2cccc3[nH]c(O)nc23)CC1 10.1016/s0960-894x(03)00387-1
1499 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.5b00638
3779 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.5b00638
536 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.5b00638
CHEMBL434 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.5b00638
DB01064 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 minsAgonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.5b00638
10100 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
44472635 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
5311 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
CHEMBL2107826 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
DB14895 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
ChEMBL 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 10.1021/acs.jmedchem.5b01372
46881980 12511 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 427 9 3 5 4.5 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1ccco1 10.1016/j.bmcl.2010.01.130
CHEMBL1078394 12511 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 427 9 3 5 4.5 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1ccco1 10.1016/j.bmcl.2010.01.130
46881651 13633 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 458 10 3 6 4.3 O=C(Cc1nc(-c2ccccc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084137 13633 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 458 10 3 6 4.3 O=C(Cc1nc(-c2ccccc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
145832533 68761 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 533 9 5 9 1.6 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(CC4SC(N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
18629731 68761 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 533 9 5 9 1.6 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(CC4SC(N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL177438 68761 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 533 9 5 9 1.6 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(CC4SC(N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
44280795 119354 0 None 97 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 507 12 3 8 3.8 CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33013 119354 0 None 97 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptorAgonist activity as increasedn cAMP production in Chinese hamster ovary (CHO)cells expressing human beta-3 adrenergic receptor
ChEMBL 507 12 3 8 3.8 CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
1499 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Concentration required to effect a 50% relaxation of rat ferret detrusor basal toneConcentration required to effect a 50% relaxation of rat ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
3779 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Concentration required to effect a 50% relaxation of rat ferret detrusor basal toneConcentration required to effect a 50% relaxation of rat ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
536 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Concentration required to effect a 50% relaxation of rat ferret detrusor basal toneConcentration required to effect a 50% relaxation of rat ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
CHEMBL434 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Concentration required to effect a 50% relaxation of rat ferret detrusor basal toneConcentration required to effect a 50% relaxation of rat ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
DB01064 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Concentration required to effect a 50% relaxation of rat ferret detrusor basal toneConcentration required to effect a 50% relaxation of rat ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
1499 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
3779 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
536 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
CHEMBL434 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
DB01064 8872 47 None -190 38 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal toneAgonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
1499 8872 47 None -338 38 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
3779 8872 47 None -338 38 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
536 8872 47 None -338 38 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
CHEMBL434 8872 47 None -338 38 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
DB01064 8872 47 None -338 38 Rat 7.1 pEC50 = 7.1 Functional
Agonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusorAgonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
44331551 113991 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 395 9 3 4 3.8 CCCN1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
CHEMBL316649 113991 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-3 adrenergic receptor
ChEMBL 395 9 3 4 3.8 CCCN1CCC(CNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/s0960-894x(02)00607-8
44298718 203866 0 None 22 3 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 386 8 1 3 4.3 CCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL56752 203866 0 None 22 3 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro agonistic activity against cloned human beta-3 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 386 8 1 3 4.3 CCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44517692 203448 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203990 203448 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL564516 203448 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
44589133 182623 0 None 1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta-3 receptor in human SK-N-MC cellsAgonist activity at adrenergic beta-3 receptor in human SK-N-MC cells
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
CHEMBL458541 182623 0 None 1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta-3 receptor in human SK-N-MC cellsAgonist activity at adrenergic beta-3 receptor in human SK-N-MC cells
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
45269853 203347 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL563872 203347 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
44127479 202958 0 None -10 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1cccc(Cl)c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561348 202958 0 None -10 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1cccc(Cl)c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
24950055 181823 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.3 Cc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1C(=O)O 10.1021/jm800222k
CHEMBL456772 181823 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.3 Cc1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc1C(=O)O 10.1021/jm800222k
44392480 71353 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 471 12 4 6 4.1 CC/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181603 71353 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
ChEMBL 471 12 4 6 4.1 CC/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44385820 66774 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 531 8 5 9 2.0 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(/C=C4\SC(N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL173472 66774 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 531 8 5 9 2.0 CS(=O)(=O)Nc1cc(C(O)CNC2CCN(c3ccc(/C=C4\SC(N)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
44386368 67107 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 599 8 4 9 3.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(N5CCCCC5)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL174442 67107 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 599 8 4 9 3.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(N5CCCCC5)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
12147062 68042 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 576 8 4 9 3.7 O=C1N=C(N2CCCCC2)S/C1=C\c1ccc(N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(01)00147-0
CHEMBL176629 68042 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 576 8 4 9 3.7 O=C1N=C(N2CCCCC2)S/C1=C\c1ccc(N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1 10.1016/s0960-894x(01)00147-0
10233153 11001 0 None 5 3 Human 8.1 pEC50 = 8.1 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 642 11 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4ccc5c(C(=O)O)cccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL100351 11001 0 None 5 3 Human 8.1 pEC50 = 8.1 Functional
Beta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptorBeta-3 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-3-adrenoceptor
ChEMBL 642 11 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4ccc5c(C(=O)O)cccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
10076548 170043 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 562 13 5 8 2.7 CCCCN(C(=O)CC(=O)O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL418600 170043 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 562 13 5 8 2.7 CCCCN(C(=O)CC(=O)O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
44402728 78752 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 608 12 4 6 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3c[nH]c4ccccc34)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL197364 78752 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 608 12 4 6 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3c[nH]c4ccccc34)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301880 205418 0 None 5370 3 Human 8.0 pEC50 = 8.0 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 596 11 3 8 6.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4o3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL57908 205418 0 None 5370 3 Human 8.0 pEC50 = 8.0 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 596 11 3 8 6.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4o3)cs2)cc1 10.1016/s0960-894x(00)00390-5
12017014 107089 0 None 102 3 Human 8.0 pEC50 = 8.0 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 608 12 3 7 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3cc(F)c(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL289316 107089 0 None 102 3 Human 8.0 pEC50 = 8.0 Functional
In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.In vitro efficacy at beta-3 adrenoceptors, quantified by measuring intracellular cAMP.
ChEMBL 608 12 3 7 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3cc(F)c(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
44579966 199397 0 None 15 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 429 9 3 4 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
CHEMBL521611 199397 0 None 15 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 429 9 3 4 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
44579925 191104 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 445 9 3 4 5.4 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1Cl 10.1016/j.bmcl.2008.08.009
CHEMBL484265 191104 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 445 9 3 4 5.4 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1Cl 10.1016/j.bmcl.2008.08.009
44377636 126876 0 None 363 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 607 12 3 6 4.5 O=C1N(Cc2ccc(F)c(F)c2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL350931 126876 0 None 363 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity towards Beta-3 adrenergic receptorAgonist activity towards Beta-3 adrenergic receptor
ChEMBL 607 12 3 6 4.5 O=C1N(Cc2ccc(F)c(F)c2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44402695 77884 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 587 12 3 6 6.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc(F)cc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
CHEMBL195409 77884 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 587 12 3 6 6.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(Cc2nc(-c3ccc(F)cc3)cs2)cc1 10.1016/j.bmcl.2005.03.119
44301618 205860 0 None 158 3 Human 8.0 pEC50 = 8.0 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 574 11 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL58798 205860 0 None 158 3 Human 8.0 pEC50 = 8.0 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 574 11 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
24949420 194894 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
CHEMBL498304 194894 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
127041559 143895 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 470 7 2 5 3.1 CCS(=O)(=O)C1CCN(C(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)CC1 10.1016/j.bmcl.2015.11.030
CHEMBL3747710 143895 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assayAgonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as reduction in cAMP level after 30 mins by LANCE TR-FRET assay
ChEMBL 470 7 2 5 3.1 CCS(=O)(=O)C1CCN(C(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)CC1 10.1016/j.bmcl.2015.11.030
24822971 102223 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2Cl)cc1 10.1021/jm701324c
CHEMBL257106 102223 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2Cl)cc1 10.1021/jm701324c
24823130 104480 0 None 38 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1F 10.1021/jm701324c
CHEMBL271367 104480 0 None 38 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1F 10.1021/jm701324c
44402687 175371 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 619 19 3 6 7.5 CCCCCCCCc1csc(CCc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
CHEMBL435914 175371 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptorEffective concentration to stimulate cAMP production in chinese hamster ovary cells expressing cloned human beta-3-adrenergic receptor
ChEMBL 619 19 3 6 7.5 CCCCCCCCc1csc(CCc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4ccccc4)cc3)cc2)n1 10.1016/j.bmcl.2005.03.119
44301866 107351 0 None 87 3 Human 8.0 pEC50 = 8.0 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 606 18 3 7 6.7 CCCCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL291593 107351 0 None 87 3 Human 8.0 pEC50 = 8.0 Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptorStimulated increase in cAMP in CHO cells expressing human beta-3 receptor
ChEMBL 606 18 3 7 6.7 CCCCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
10278987 109738 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 506 10 4 9 1.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1OC 10.1016/s0960-894x(03)00387-1
CHEMBL306430 109738 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 506 10 4 9 1.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c(O)nc34)CC2)cc1OC 10.1016/s0960-894x(03)00387-1
135995975 134589 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 704 11 5 10 4.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NC5CCN(Cc6ccccc6)CC5)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL366395 134589 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 704 11 5 10 4.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(/C=C4\SC(NC5CCN(Cc6ccccc6)CC5)=NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
10205463 12274 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 470 11 5 6 3.0 CC(C)NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107633 12274 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
ChEMBL 470 11 5 6 3.0 CC(C)NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44377536 62193 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 426 7 3 7 2.3 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4cccnc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL161950 62193 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
ChEMBL 426 7 3 7 2.3 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4cccnc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
24822313 102858 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 395 8 3 3 4.6 O=C(O)c1cccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
CHEMBL260100 102858 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 395 8 3 3 4.6 O=C(O)c1cccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
44268275 26385 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 484 14 4 6 3.3 O=S(=O)(CCCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13003 26385 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against cloned human beta-3 adrenergic receptorAgonist activity against cloned human beta-3 adrenergic receptor
ChEMBL 484 14 4 6 3.3 O=S(=O)(CCCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
24886595 24418 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccc(F)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258370 24418 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccc(F)cc1 10.1016/j.bmcl.2010.08.039
10627031 106687 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 578 13 7 9 1.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL286126 106687 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 578 13 7 9 1.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
44309633 175957 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 549 9 3 5 5.1 CC(C)(C)Cc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL440576 175957 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
ChEMBL 549 9 3 5 5.1 CC(C)(C)Cc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
45270673 202203 0 None -58 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203992 202203 0 None -58 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552253 202203 0 None -58 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
101136734 67123 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 522 8 4 7 2.7 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44386051 67123 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 522 8 4 7 2.7 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
88054051 67123 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 522 8 4 7 2.7 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
CHEMBL174534 67123 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.Beta 3-adrenergic receptor agonistic activity, evaluated by measurement of cAMP accumulation in CHO cells.
ChEMBL 522 8 4 7 2.7 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
10271144 20934 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 380 10 3 6 1.0 CN(C)S(=O)(=O)Nc1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL1198530 20934 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 380 10 3 6 1.0 CN(C)S(=O)(=O)Nc1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL544338 20934 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 380 10 3 6 1.0 CN(C)S(=O)(=O)Nc1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(04)00462-7
46881528 14033 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 389 8 3 4 3.8 Cc1ccc(C)c(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1085897 14033 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 389 8 3 4 3.8 Cc1ccc(C)c(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/j.bmcl.2010.01.130
11244811 99064 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 342 6 3 2 4.4 Cc1cccc2[nH]cc(CC(C)NCC(O)c3cccc(Cl)c3)c12 10.1016/s0960-894x(03)00073-8
CHEMBL24269 99064 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 342 6 3 2 4.4 Cc1cccc2[nH]cc(CC(C)NCC(O)c3cccc(Cl)c3)c12 10.1016/s0960-894x(03)00073-8
52947060 24355 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 474 8 2 7 4.7 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258144 24355 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 474 8 2 7 4.7 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
44127478 201993 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 435 11 5 6 2.6 NC(C(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL550743 201993 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 435 11 5 6 2.6 NC(C(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
44127048 202134 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 436 11 5 6 2.6 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(O)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL551832 202134 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 436 11 5 6 2.6 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(O)c1ccccc1 10.1016/j.ejmech.2009.01.022
24936883 24103 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257324 24103 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
46881872 14519 0 None -1 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 411 10 4 7 2.6 CNc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
CHEMBL1089052 14519 0 None -1 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assayAgonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
ChEMBL 411 10 4 7 2.6 CNc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
10697841 169648 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 546 9 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N4CCC[C@H]4C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL417325 169648 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor.
ChEMBL 546 9 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N4CCC[C@H]4C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
10222907 20660 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 404 9 3 5 2.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)N1CCCCC1 10.1016/s0960-894x(04)00462-7
CHEMBL1196159 20660 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 404 9 3 5 2.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)N1CCCCC1 10.1016/s0960-894x(04)00462-7
CHEMBL556022 20660 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 404 9 3 5 2.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)N1CCCCC1 10.1016/s0960-894x(04)00462-7
10295131 15108 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 411 9 2 4 2.4 CN(C)S(=O)(=O)N(C)c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(04)00462-7
CHEMBL109288 15108 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptorAgonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
ChEMBL 411 9 2 4 2.4 CN(C)S(=O)(=O)N(C)c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(04)00462-7
52943969 24567 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 517 9 3 8 4.3 CC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258825 24567 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 517 9 3 8 4.3 CC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
3687256 13606 7 None -3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
ChEMBL 500 8 1 5 5.0 Cc1ccc(C(C)C)c(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1083994 13606 7 None -3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta3 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
ChEMBL 500 8 1 5 5.0 Cc1ccc(C(C)C)c(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
24937140 24456 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 3 8 3.8 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258483 24456 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 3 8 3.8 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
52946430 24597 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 517 9 3 8 3.7 CNC(=O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258940 24597 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 517 9 3 8 3.7 CNC(=O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
10391011 21644 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Agonistic activity against Beta-3 adrenergic receptor in rat colonAgonistic activity against Beta-3 adrenergic receptor in rat colon
ChEMBL 447 6 4 6 2.5 O=C(O)C1(C(=O)O)Oc2cc3c(cc2O1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC3 10.1016/0960-894X(95)00483-A
CHEMBL1207626 21644 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Agonistic activity against Beta-3 adrenergic receptor in rat colonAgonistic activity against Beta-3 adrenergic receptor in rat colon
ChEMBL 447 6 4 6 2.5 O=C(O)C1(C(=O)O)Oc2cc3c(cc2O1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC3 10.1016/0960-894X(95)00483-A
CHEMBL421193 21644 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Agonistic activity against Beta-3 adrenergic receptor in rat colonAgonistic activity against Beta-3 adrenergic receptor in rat colon
ChEMBL 447 6 4 6 2.5 O=C(O)C1(C(=O)O)Oc2cc3c(cc2O1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CCC3 10.1016/0960-894X(95)00483-A
52948792 24492 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 488 9 2 7 4.9 CCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258596 24492 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 488 9 2 7 4.9 CCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
54669764 72266 0 None - 0 Human 7.0 pKd = 7.0 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830491 72266 0 None - 0 Human 7.0 pKd = 7.0 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
54757027 72265 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830490 72265 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54756928 72262 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830487 72262 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
54756927 72261 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830486 72261 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
2303 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
4946 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
564 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
63 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
91536 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL27 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL452861 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
DB00571 9961 68 None -165 20 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
54758320 72292 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830620 72292 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
123686 8762 51 None -12302 3 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
12581 8762 51 None -12302 3 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
CHEMBL11268 8762 51 None -12302 3 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
155774 10868 40 None -2041 3 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2848 10868 40 None -2041 3 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
538 10868 40 None -2041 3 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
CHEMBL75753 10868 40 None -2041 3 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
DB13781 10868 40 None -2041 3 Human 4.7 pKd = 4.7 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
54757229 72289 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830617 72289 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54758417 72260 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830485 72260 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
56598832 95043 0 None -4365 3 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 95043 0 None -4365 3 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
54758415 72293 0 None - 0 Human 6.5 pKd = 6.5 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830621 72293 0 None - 0 Human 6.5 pKd = 6.5 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
54757129 72268 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830493 72268 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
2685 7677 21 None - 1 Human 5.3 pKd = 5.3 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
541 7677 21 None - 1 Human 5.3 pKd = 5.3 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
CHEMBL280822 7677 21 None - 1 Human 5.3 pKd = 5.3 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
54757126 72267 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830492 72267 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54757331 72291 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830619 72291 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
66653268 95026 0 None -3311 3 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
CHEMBL2348201 95026 0 None -3311 3 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
54757232 72290 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830618 72290 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54756929 72263 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830488 72263 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
137 7158 52 None - 8 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
2119 7158 52 None - 8 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
563 7158 52 None - 8 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
66368 7158 52 None - 8 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
CHEMBL266195 7158 52 None - 8 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
DB00866 7158 52 None - 8 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
54757026 72264 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830489 72264 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
2419 10236 84 None -416 14 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 10236 84 None -416 14 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 10236 84 None -416 14 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 10236 84 None -416 14 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 10236 84 None -416 14 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
10184665 10763 51 None -40 10 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
4799 10763 51 None -40 10 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
7353 10763 51 None -40 10 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
CHEMBL1198857 10763 51 None -40 10 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
DB09082 10763 51 None -40 10 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
688570 193640 24 None 1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 287 6 4 4 2.4 C[C@@H](NCCc1ccc(O)cc1)[C@@H](O)c1ccc(O)cc1 None
CHEMBL489553 193640 24 None 1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 287 6 4 4 2.4 C[C@@H](NCCc1ccc(O)cc1)[C@@H](O)c1ccc(O)cc1 None
10100 10759 30 None -23 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
44472635 10759 30 None -23 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
5311 10759 30 None -23 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
CHEMBL2107826 10759 30 None -23 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
DB14895 10759 30 None -23 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
443372 17006 26 None -2 9 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL1160723 17006 26 None -2 9 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL2062275 17006 26 None -2 9 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
3083544 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1200811 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1363 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1951071 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL605993 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
3083544 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1200811 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1363 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1951071 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL605993 33582 51 None -16 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
Drug Central 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
4382 9317 0 None 1 6 Human 8.1 pEC50 = 8.1 Functional
cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorcAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
Drug Central 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O None
7445 9317 0 None 1 6 Human 8.1 pEC50 = 8.1 Functional
cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorcAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
Drug Central 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O None
9865528 9317 0 None 1 6 Human 8.1 pEC50 = 8.1 Functional
cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorcAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
Drug Central 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O None
CHEMBL2095212 9317 0 None 1 6 Human 8.1 pEC50 = 8.1 Functional
cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorcAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
Drug Central 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O None
DB08893 9317 0 None 1 6 Human 8.1 pEC50 = 8.1 Functional
cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptorcAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
Drug Central 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O None
10100 10759 30 None -4 4 Dog 8.1 pEC50 = 8.1 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
44472635 10759 30 None -4 4 Dog 8.1 pEC50 = 8.1 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
5311 10759 30 None -4 4 Dog 8.1 pEC50 = 8.1 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
CHEMBL2107826 10759 30 None -4 4 Dog 8.1 pEC50 = 8.1 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
DB14895 10759 30 None -4 4 Dog 8.1 pEC50 = 8.1 Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
1499 8872 47 None -190 38 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 None -190 38 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 None -190 38 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 None -190 38 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 None -190 38 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
10100 10759 30 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Mechanism of ActionMechanism of Action
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
44472635 10759 30 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Mechanism of ActionMechanism of Action
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
5311 10759 30 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Mechanism of ActionMechanism of Action
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
CHEMBL2107826 10759 30 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Mechanism of ActionMechanism of Action
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
DB14895 10759 30 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Mechanism of ActionMechanism of Action
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
10100 10759 30 None -1 4 Rhesus macaque 8.0 pEC50 = 8.0 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
44472635 10759 30 None -1 4 Rhesus macaque 8.0 pEC50 = 8.0 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
5311 10759 30 None -1 4 Rhesus macaque 8.0 pEC50 = 8.0 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
CHEMBL2107826 10759 30 None -1 4 Rhesus macaque 8.0 pEC50 = 8.0 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
DB14895 10759 30 None -1 4 Rhesus macaque 8.0 pEC50 = 8.0 Functional
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assayAgonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Drug Central 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O None
3931 9028 48 None 691 4 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 20590599
9829836 9028 48 None 691 4 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 20590599
CHEMBL12998 9028 48 None 691 4 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 20590599
2176 9901 68 None -91 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
4828 9901 68 None -91 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
91 9901 68 None -91 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
CHEMBL500 9901 68 None -91 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
DB00960 9901 68 None -91 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
1028 7079 71 None -4 19 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
139148732 7079 71 None -4 19 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
479 7079 71 None -4 19 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
5816 7079 71 None -4 19 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
CHEMBL679 7079 71 None -4 19 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
DB00668 7079 71 None -4 19 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
12578 7723 61 None -186 3 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 20590599
2755 7723 61 None -186 3 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 20590599
CHEMBL1374751 7723 61 None -186 3 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 20590599
10100 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
44472635 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
5311 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
CHEMBL2107826 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
DB14895 10759 30 None -23 4 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
3468 10281 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 12 4 6 4.2 O[C@H](COc1ccc(cc1)O)CNC1(CCCC1)Cc1ccc(cc1)OCP(=O)(c1ccccc1)O 11959793
9958026 10281 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 12 4 6 4.2 O[C@H](COc1ccc(cc1)O)CNC1(CCCC1)Cc1ccc(cc1)OCP(=O)(c1ccccc1)O 11959793
1960 9632 67 None -1 19 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20590599
439260 9632 67 None -1 19 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20590599
505 9632 67 None -1 19 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20590599
CHEMBL1437 9632 67 None -1 19 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20590599
DB00368 9632 67 None -1 19 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20590599
1499 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
3779 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
536 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
CHEMBL434 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
DB01064 8872 47 None -190 38 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
567 7512 16 None -2 7 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 20590599
9841972 7512 16 None -2 7 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 20590599
CHEMBL284782 7512 16 None -2 7 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 20590599
4382 9317 0 None -1 6 Mouse 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
7445 9317 0 None -1 6 Mouse 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
9865528 9317 0 None -1 6 Mouse 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
CHEMBL2095212 9317 0 None -1 6 Mouse 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
DB08893 9317 0 None -1 6 Mouse 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
1155 8410 53 None 1 11 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
3343 8410 53 None 1 11 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
557 8410 53 None 1 11 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
CHEMBL32800 8410 53 None 1 11 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
DB01288 8410 53 None 1 11 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
4382 9317 0 None -3 6 Rat 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
7445 9317 0 None -3 6 Rat 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
9865528 9317 0 None -3 6 Rat 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
CHEMBL2095212 9317 0 None -3 6 Rat 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
DB08893 9317 0 None -3 6 Rat 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
4382 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
4382 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 23239087
4382 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
4382 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 35693456
7445 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
7445 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 23239087
7445 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
7445 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 35693456
9865528 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
9865528 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 23239087
9865528 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
9865528 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 35693456
CHEMBL2095212 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
CHEMBL2095212 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 23239087
CHEMBL2095212 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
CHEMBL2095212 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 35693456
DB08893 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
DB08893 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 23239087
DB08893 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
DB08893 9317 0 None 1 6 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 35693456
10028830 9026 40 None 323 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
3932 9026 40 None 323 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
CHEMBL4238084 9026 40 None 323 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
9512 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
9512 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 23263450
9512 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 26808167
9887812 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
9887812 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 23263450
9887812 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 26808167
CHEMBL208427 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
CHEMBL208427 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 23263450
CHEMBL208427 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 26808167
DB06190 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
DB06190 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 23263450
DB06190 10408 42 None 380 3 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 26808167
4382 9317 0 None -1 6 Mouse 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
7445 9317 0 None -1 6 Mouse 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
9865528 9317 0 None -1 6 Mouse 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
CHEMBL2095212 9317 0 None -1 6 Mouse 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
DB08893 9317 0 None -1 6 Mouse 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 32813332
487 7580 71 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
569 7580 71 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
71739 7580 71 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
CHEMBL324665 7580 71 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
16118894 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 9873496
3467 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 9873496
CHEMBL276257 9023 5 None 75 3 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 9873496
10100 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
10100 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 27965369
10100 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 35693456
44472635 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
44472635 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 27965369
44472635 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 35693456
5311 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
5311 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 27965369
5311 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 35693456
CHEMBL2107826 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
CHEMBL2107826 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 27965369
CHEMBL2107826 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 35693456
DB14895 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 26709102
DB14895 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 27965369
DB14895 10759 30 None 1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 3 6 2.8 O=C([C@@H]1CCc2n1c(=O)ccn2)Nc1ccc(cc1)C[C@@H]1CC[C@@H](N1)[C@@H](c1ccccc1)O 35693456
146015362 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 16601951
146015362 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
3462 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 16601951
3462 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
5486546 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 16601951
5486546 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
CHEMBL1204876 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 16601951
CHEMBL1204876 7734 10 None 15 5 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
11962616 7009 14 None -3388 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
9326 7009 14 None -3388 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
CHEMBL3039530 7009 14 None -3388 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
DB12100 7009 14 None -3388 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
10028830 9026 40 None 323 3 Human 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 18684840
3932 9026 40 None 323 3 Human 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 18684840
CHEMBL4238084 9026 40 None 323 3 Human 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 18684840




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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3333 46942 111 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 4 1 5 4.0 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc(Cl)c1Cl 10.1038/s41467-023-40064-9
CHEMBL1480 46942 111 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 4 1 5 4.0 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc(Cl)c1Cl 10.1038/s41467-023-40064-9
1353 8692 93 None - 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None - 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None - 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None - 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None - 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
53232 195404 95 None - 2 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL503 195404 95 None - 2 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
2351 11072 49 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 11072 49 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 11072 49 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
2585 7590 103 None -16 22 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 7590 103 None -16 22 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 7590 103 None -16 22 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 7590 103 None -16 22 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 7590 103 None -16 22 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
445643 104164 69 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
CHEMBL269732 104164 69 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
2274 9947 58 None - 31 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 9947 58 None - 31 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 9947 58 None - 31 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 9947 58 None - 31 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 9947 58 None - 31 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
392622 63086 95 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 63086 95 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
11626560 207716 94 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 207716 94 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
3339 210420 117 None -10 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL672 210420 117 None -10 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1 10.1038/s41467-023-40064-9
2405 7452 76 None -32 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1038/s41467-023-40064-9
380 7452 76 None -32 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1038/s41467-023-40064-9
7129 7452 76 None -32 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL645 7452 76 None -32 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1038/s41467-023-40064-9
DB00612 7452 76 None -32 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1038/s41467-023-40064-9
4507 187457 101 None - 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 360 5 1 7 2.6 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL475534 187457 101 None - 4 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 360 5 1 7 2.6 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
100 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
3157 8252 71 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 8252 71 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 8252 71 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 8252 71 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 8252 71 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
9687 192114 25 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 11 1.7 CCCC(=O)Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1OC(=O)CCC 10.1038/s41467-023-40064-9
CHEMBL1522836 192114 25 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 11 1.7 CCCC(=O)Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1OC(=O)CCC 10.1038/s41467-023-40064-9
CHEMBL485980 192114 25 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 11 1.7 CCCC(=O)Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1OC(=O)CCC 10.1038/s41467-023-40064-9
5328940 106992 107 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 106992 107 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
5472 212597 75 None - 3 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 212597 75 None - 3 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 212597 75 None - 3 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
31101 7516 40 None - 35 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None - 35 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None - 35 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None - 35 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None - 35 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
4054 212280 72 None - 36 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 10.1038/s41467-023-40064-9
CHEMBL1699 212280 72 None - 36 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 10.1038/s41467-023-40064-9
CHEMBL807 212280 72 None - 36 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 10.1038/s41467-023-40064-9
2105 9828 37 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 9828 37 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 9828 37 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 9828 37 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 9828 37 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
1212 8443 50 None -630 65 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 8443 50 None -630 65 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 8443 50 None -630 65 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 8443 50 None -630 65 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 8443 50 None -630 65 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2726 7706 68 None - 72 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 7706 68 None - 72 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 7706 68 None - 72 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 7706 68 None - 72 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 7706 68 None - 72 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
448537 167029 89 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 167029 89 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
5284616 168406 55 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 914 6 3 13 6.2 CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C 10.1038/s41467-023-40064-9
CHEMBL413 168406 55 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 914 6 3 13 6.2 CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C 10.1038/s41467-023-40064-9
176 7186 66 None -10 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 7186 66 None -10 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 7186 66 None -10 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 7186 66 None -10 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 7186 66 None -10 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
10531 8202 21 None - 24 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None - 24 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None - 24 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None - 24 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None - 24 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
2162 48288 100 None - 6 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 48288 100 None - 6 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
44400012 212608 83 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 235 4 6 4 -1.7 NCCC(O)(P(=O)(O)O)P(=O)(O)O 10.1038/s41467-023-40064-9
4674 212608 83 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 235 4 6 4 -1.7 NCCC(O)(P(=O)(O)O)P(=O)(O)O 10.1038/s41467-023-40064-9
CHEMBL834 212608 83 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 235 4 6 4 -1.7 NCCC(O)(P(=O)(O)O)P(=O)(O)O 10.1038/s41467-023-40064-9
135398735 143746 32 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 143746 32 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 143746 32 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
5991 210698 72 None - 5 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL691 210698 72 None - 5 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
16220172 79818 95 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 2 3 3 5.1 CC(C)(C)c1cc(C(C)(C)C)c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O 10.1038/s41467-023-40064-9
CHEMBL2010601 79818 95 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 2 3 3 5.1 CC(C)(C)c1cc(C(C)(C)C)c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O 10.1038/s41467-023-40064-9
16362 9899 71 None - 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None - 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None - 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None - 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None - 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
54454 12030 88 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 12030 88 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
2662 18156 131 None 1 30 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL118 18156 131 None 1 30 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
1016 10519 78 None -33 35 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 10519 78 None -33 35 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 10519 78 None -33 35 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 10519 78 None -33 35 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 10519 78 None -33 35 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 10519 78 None -33 35 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
242 7258 124 None - 51 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None - 51 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None - 51 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None - 51 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None - 51 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
3672 199312 136 None - 27 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 10.1038/s41467-023-40064-9
CHEMBL521 199312 136 None - 27 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 10.1038/s41467-023-40064-9
2303 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 9961 68 None -213 26 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
2600 10551 74 None - 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None - 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None - 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None - 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None - 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
3114 196706 71 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 339 8 1 3 3.4 CC(C)N(CCC(C(N)=O)(c1ccccc1)c1ccccn1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL517 196706 71 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 339 8 1 3 3.4 CC(C)N(CCC(C(N)=O)(c1ccccc1)c1ccccn1)C(C)C 10.1038/s41467-023-40064-9
1605 9121 117 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
3957 9121 117 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
7216 9121 117 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
CHEMBL998 9121 117 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
DB00455 9121 117 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
2812 11551 101 None -35 34 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL104 11551 101 None -35 34 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1038/s41467-023-40064-9
2351 10059 64 None - 21 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
2820 10059 64 None - 21 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
5035 10059 64 None - 21 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
CHEMBL81 10059 64 None - 21 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
DB00481 10059 64 None - 21 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
1890 9535 49 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 9535 49 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 9535 49 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 9535 49 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 9535 49 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human ADRB3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
44303556 109094 0 None - 0 Human 10.2 pEC50 = 10.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 388 9 4 4 3.2 O=C(O)COc1cccc2cc(CCNC[C@H](O)c3cccc(Cl)c3)[nH]c12 10.1021/jm980521l
CHEMBL303537 109094 0 None - 0 Human 10.2 pEC50 = 10.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 388 9 4 4 3.2 O=C(O)COc1cccc2cc(CCNC[C@H](O)c3cccc(Cl)c3)[nH]c12 10.1021/jm980521l
6916441 106103 1 None - 0 Human 10.2 pEC50 = 10.2 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL282190 106103 1 None - 0 Human 10.2 pEC50 = 10.2 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
45101537 202053 0 None - 0 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human adrenergic beta3 receptor by radioligand binding assayAgonist activity at human adrenergic beta3 receptor by radioligand binding assay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm200371q
CHEMBL551272 202053 0 None - 0 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human adrenergic beta3 receptor by radioligand binding assayAgonist activity at human adrenergic beta3 receptor by radioligand binding assay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm200371q
11432806 72971 0 None 12 3 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL184407 72971 0 None 12 3 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44396715 74225 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL189081 74225 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44396531 73609 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL186135 73609 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
137649223 163901 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 552 8 2 8 3.8 Cc1noc(-c2cccc(CN3CCN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)CC3)n2)n1 10.1016/j.bmcl.2016.12.033
CHEMBL4074920 163901 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 552 8 2 8 3.8 Cc1noc(-c2cccc(CN3CCN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)CC3)n2)n1 10.1016/j.bmcl.2016.12.033
9906822 168816 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL416012 168816 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1007/s00044-009-9257-x
3931 9028 48 None - 2 Human 9.4 pEC50 = 9.4 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm980521l
9829836 9028 48 None - 2 Human 9.4 pEC50 = 9.4 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm980521l
CHEMBL12998 9028 48 None - 2 Human 9.4 pEC50 = 9.4 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm980521l
76333795 92090 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
CHEMBL2260985 92090 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
44396513 73497 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL185660 73497 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
76315638 92091 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260986 92091 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
44396596 130078 0 None 1 3 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL361505 130078 0 None 1 3 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
44396530 73862 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL187317 73862 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
44396736 73642 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL186271 73642 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44396577 73726 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL186676 73726 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44396779 73835 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL187209 73835 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44396532 73530 0 None 1 3 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL185836 73530 0 None 1 3 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
10258518 108728 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 633 17 3 8 6.8 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL301231 108728 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 633 17 3 8 6.8 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
76322965 92094 0 None - 0 Human 9.0 pEC50 = 9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 511 9 3 7 4.5 C[C@H](Cc1cn2c3c(cccc13)OCCC2)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL2260989 92094 0 None - 0 Human 9.0 pEC50 = 9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 511 9 3 7 4.5 C[C@H](Cc1cn2c3c(cccc13)OCCC2)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
76315637 92089 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 607 12 4 10 4.2 CCOC(=O)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL2260984 92089 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 607 12 4 10 4.2 CCOC(=O)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
44392457 172736 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL425161 172736 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
76319327 92101 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 584 14 4 7 4.5 CCN(CC)C(=O)COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL2261203 92101 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 584 14 4 7 4.5 CCN(CC)C(=O)COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
137656598 166372 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 525 9 2 8 2.3 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2nnn(CC(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
CHEMBL4103112 166372 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 525 9 2 8 2.3 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2nnn(CC(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
137634334 163159 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 542 8 2 7 3.2 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2ncn(CC(F)(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
CHEMBL4066314 163159 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 542 8 2 7 3.2 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2ncn(CC(F)(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
44396568 74060 0 None 9 3 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL188196 74060 0 None 9 3 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44396659 74138 0 None 6 3 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1021/acs.jmedchem.6b01197
CHEMBL188622 74138 0 None 6 3 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1021/acs.jmedchem.6b01197
137648464 164768 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 543 8 2 8 2.6 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2nnn(CC(F)(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
CHEMBL4085173 164768 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 543 8 2 8 2.6 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2nnn(CC(F)(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
44392575 71146 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL181300 71146 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
44349379 25300 0 None - 0 Human 8.0 pEC50 = 8 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 462 12 5 8 2.6 NC(=O)c1cccc(N/C(=C/[N+](=O)[O-])Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/s0960-894x(00)00669-7
CHEMBL127451 25300 0 None - 0 Human 8.0 pEC50 = 8 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 462 12 5 8 2.6 NC(=O)c1cccc(N/C(=C/[N+](=O)[O-])Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/s0960-894x(00)00669-7
44461468 112405 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 608 17 4 9 3.7 CCCCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL312364 112405 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 608 17 4 9 3.7 CCCCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
44461485 113720 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 564 15 3 9 3.7 CCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL314893 113720 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 564 15 3 9 3.7 CCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
10112732 23584 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 418 8 4 5 3.3 N#CN/C(=N\c1cccc(F)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL124668 23584 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 418 8 4 5 3.3 N#CN/C(=N\c1cccc(F)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
10119061 24728 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1ccc(I)cc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL126055 24728 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1ccc(I)cc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
10282871 23321 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3cc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)ccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL123745 23321 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3cc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)ccc32)n1 10.1016/s0960-894x(00)00669-7
44349237 170218 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 511 13 4 8 5.3 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(Oc2ccccc2)c1 10.1016/s0960-894x(00)00669-7
CHEMBL419787 170218 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 511 13 4 8 5.3 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(Oc2ccccc2)c1 10.1016/s0960-894x(00)00669-7
2419 10236 84 None -53 6 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
5152 10236 84 None -53 6 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
559 10236 84 None -53 6 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
CHEMBL1263 10236 84 None -53 6 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
DB00938 10236 84 None -53 6 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
45381932 129314 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 432 10 4 6 2.8 CC(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL3601305 129314 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 432 10 4 6 2.8 CC(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.6b01197
44461706 212702 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 579 15 3 7 4.1 CCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL84117 212702 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 579 15 3 7 4.1 CCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
10416656 25381 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3c(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL127656 25381 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3c(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cccc32)n1 10.1016/s0960-894x(00)00669-7
9917962 174735 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL431678 174735 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44461567 110951 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 579 15 3 7 4.1 CCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL309673 110951 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 579 15 3 7 4.1 CCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
44461488 212154 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 606 13 3 7 3.0 O=C(CCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O)N1CCCC1 10.1016/s0960-894x(03)00491-8
CHEMBL79915 212154 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 606 13 3 7 3.0 O=C(CCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O)N1CCCC1 10.1016/s0960-894x(03)00491-8
44349629 25296 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL127422 25296 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
45381852 129300 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL3601204 129300 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.6b01197
10347866 91782 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL22386 91782 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
44461719 212643 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 641 14 3 6 5.0 O=C1N(CCCC(F)(F)C(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(03)00491-8
CHEMBL83754 212643 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 641 14 3 6 5.0 O=C1N(CCCC(F)(F)C(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(03)00491-8
44349356 123762 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc2ccccc12 10.1016/s0960-894x(00)00669-7
CHEMBL338748 123762 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc2ccccc12 10.1016/s0960-894x(00)00669-7
44461490 112179 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 594 17 4 7 4.8 CCCCCCCCN1NCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL311731 112179 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 594 17 4 7 4.8 CCCCCCCCN1NCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
10160636 120275 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 443 9 5 6 2.2 N#CN/C(=N\c1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(C(N)=O)c1 10.1016/s0960-894x(00)00669-7
CHEMBL332010 120275 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 443 9 5 6 2.2 N#CN/C(=N\c1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(C(N)=O)c1 10.1016/s0960-894x(00)00669-7
44308088 210376 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL66936 210376 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
76315639 92092 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(C(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260987 92092 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(C(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
51349173 163261 8 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 444 10 4 6 2.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CCC4)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL4067502 163261 8 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 444 10 4 6 2.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CCC4)c3)ccc12 10.1021/acs.jmedchem.6b01197
137640335 163767 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 481 11 4 7 2.1 CCS(=O)(=O)Nc1cccc([C@@H](O)CNCCc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1021/acs.jmedchem.6b01197
CHEMBL4073098 163767 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 481 11 4 7 2.1 CCS(=O)(=O)Nc1cccc([C@@H](O)CNCCc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1021/acs.jmedchem.6b01197
44461489 212131 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 591 13 3 6 4.3 O=C1N(CCCC(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(03)00491-8
CHEMBL79675 212131 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 591 13 3 6 4.3 O=C1N(CCCC(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(03)00491-8
10099459 212475 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL82296 212475 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
44349357 166688 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1ccc2ccccc2c1 10.1016/s0960-894x(00)00669-7
CHEMBL410702 166688 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1ccc2ccccc2c1 10.1016/s0960-894x(00)00669-7
9810596 23571 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 734 11 4 9 8.0 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc2cc(CCNC[C@H](O)c3cccnc3)ccc2c1 10.1016/s0960-894x(00)00669-7
CHEMBL124597 23571 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 734 11 4 9 8.0 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc2cc(CCNC[C@H](O)c3cccnc3)ccc2c1 10.1016/s0960-894x(00)00669-7
11318107 113165 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3126386 113165 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3139364 113165 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
15523859 212712 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL84190 212712 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
137653127 165679 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 552 8 2 8 3.8 Cc1nnc(-c2cccc(CN3CCN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)CC3)n2)o1 10.1016/j.bmcl.2016.12.033
CHEMBL4095361 165679 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 552 8 2 8 3.8 Cc1nnc(-c2cccc(CN3CCN(C(=O)c4ccc(C[C@@H]5CC[C@H]([C@H](O)c6ccccc6)N5)cc4)CC3)n2)o1 10.1016/j.bmcl.2016.12.033
44392542 72636 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1007/s00044-009-9257-x
CHEMBL183552 72636 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1007/s00044-009-9257-x
137643636 164960 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 524 9 2 7 2.9 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2ncn(CC(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
CHEMBL4087670 164960 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 524 9 2 7 2.9 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2ncn(CC(F)F)n2)CC1 10.1016/j.bmcl.2016.12.033
67972431 163770 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 470 7 2 5 3.4 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2ccccn2)CC1 10.1016/j.bmcl.2016.12.033
CHEMBL4073137 163770 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 470 7 2 5 3.4 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2ccccn2)CC1 10.1016/j.bmcl.2016.12.033
19360456 195485 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1 10.1021/jm900364m
CHEMBL504479 195485 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1 10.1021/jm900364m
44186438 193125 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL487508 193125 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
19360455 193854 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL491251 193854 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
567 7512 16 None -1 5 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
9841972 7512 16 None -1 5 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
CHEMBL284782 7512 16 None -1 5 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
10135864 129296 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL3601200 129296 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.6b01197
44349378 25297 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 545 11 4 7 4.2 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(I)c1 10.1016/s0960-894x(00)00669-7
CHEMBL127428 25297 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 545 11 4 7 4.2 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(I)c1 10.1016/s0960-894x(00)00669-7
146015362 7734 10 None -8 3 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
3462 7734 10 None -8 3 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
5486546 7734 10 None -8 3 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
CHEMBL1204876 7734 10 None -8 3 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
11270071 105766 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL279931 105766 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
3083544 33582 51 None -43 5 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL1200811 33582 51 None -43 5 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL1363 33582 51 None -43 5 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL1951071 33582 51 None -43 5 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL605993 33582 51 None -43 5 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
10370605 113210 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
CHEMBL3126385 113210 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
CHEMBL3139615 113210 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
11318358 113209 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3126387 113209 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3139613 113209 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
10206782 23627 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 492 10 4 6 4.9 N#CN/C(=N\c1cccc(Oc2ccccc2)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL124863 23627 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 492 10 4 6 4.9 N#CN/C(=N\c1cccc(Oc2ccccc2)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44461718 212642 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL83753 212642 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
10437614 107719 12 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1007/s00044-009-9257-x
CHEMBL294042 107719 12 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1007/s00044-009-9257-x
45380471 165139 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 466 10 4 6 3.4 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccccc4)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL4089669 165139 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 466 10 4 6 3.4 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)c4ccccc4)c3)ccc12 10.1021/acs.jmedchem.6b01197
9826916 209411 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 491 11 5 8 2.9 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(O)nc12 10.1021/jm980521l
CHEMBL61275 209411 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 491 11 5 8 2.9 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(O)nc12 10.1021/jm980521l
9820697 209505 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 370 8 4 7 1.6 Cn1c(C(=O)O)cc2cc(OCCNC[C@H](O)c3ccc(N)nc3)ccc21 10.1021/jm980521l
CHEMBL61817 209505 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 370 8 4 7 1.6 Cn1c(C(=O)O)cc2cc(OCCNC[C@H](O)c3ccc(N)nc3)ccc21 10.1021/jm980521l
44349323 23568 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 437 11 4 7 3.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(F)c1 10.1016/s0960-894x(00)00669-7
CHEMBL124584 23568 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 437 11 4 7 3.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(F)c1 10.1016/s0960-894x(00)00669-7
68155065 165049 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 458 10 4 6 3.3 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CCCC4)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL4088750 165049 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 458 10 4 6 3.3 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CCCC4)c3)ccc12 10.1021/acs.jmedchem.6b01197
10482960 113166 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3126383 113166 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3139365 113166 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
44349367 23693 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 487 11 4 7 4.9 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(00)00669-7
CHEMBL125246 23693 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 487 11 4 7 4.9 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(00)00669-7
44392558 72029 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL182770 72029 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
443372 17006 26 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm401532g
CHEMBL1160723 17006 26 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm401532g
CHEMBL2062275 17006 26 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm401532g
10347461 113057 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
CHEMBL3126384 113057 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
CHEMBL3139025 113057 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
10053159 113058 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
CHEMBL3124955 113058 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
CHEMBL3139033 113058 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
76329060 113213 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
CHEMBL3126381 113213 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
CHEMBL3139685 113213 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
76315640 92093 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 575 12 3 7 5.8 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)cn(Cc3ccccc3)c12 10.1007/s00044-009-9257-x
CHEMBL2260988 92093 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 575 12 3 7 5.8 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)cn(Cc3ccccc3)c12 10.1007/s00044-009-9257-x
44461705 212634 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL83698 212634 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
10138809 175864 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL439794 175864 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
51347282 164376 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 430 10 4 6 2.5 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CC4)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL4080868 164376 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 430 10 4 6 2.5 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CC4)c3)ccc12 10.1021/acs.jmedchem.6b01197
137631487 163061 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 489 8 2 8 2.0 CCn1nnc(CN2CCN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)CC2)n1 10.1016/j.bmcl.2016.12.033
CHEMBL4065251 163061 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 489 8 2 8 2.0 CCn1nnc(CN2CCN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)CC2)n1 10.1016/j.bmcl.2016.12.033
137655838 165450 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 515 9 2 8 2.4 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2nnn(CC3CC3)n2)CC1 10.1016/j.bmcl.2016.12.033
CHEMBL4092912 165450 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human beta3 adrenergic receptorAgonist activity at human beta3 adrenergic receptor
ChEMBL 515 9 2 8 2.4 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCN(Cc2nnn(CC3CC3)n2)CC1 10.1016/j.bmcl.2016.12.033
44349588 123740 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 628 16 4 7 8.0 CCCCCCCCc1csc(N2CCc3cc(N/C(S)=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL338664 123740 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 628 16 4 7 8.0 CCCCCCCCc1csc(N2CCc3cc(N/C(S)=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
9927453 103462 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL26393 103462 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
44461496 110944 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 594 17 4 7 4.8 CCCCCCCCN1CNN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
CHEMBL309628 110944 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 594 17 4 7 4.8 CCCCCCCCN1CNN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(03)00491-8
45381932 129314 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at rat beta3-adrenergic receptorAgonist activity at rat beta3-adrenergic receptor
ChEMBL 432 10 4 6 2.8 CC(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601305 129314 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at rat beta3-adrenergic receptorAgonist activity at rat beta3-adrenergic receptor
ChEMBL 432 10 4 6 2.8 CC(C)c1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
10101116 21304 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1cccc2c1CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL120238 21304 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1cccc2c1CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44349646 23641 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3ccc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL124929 23641 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3ccc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cc32)n1 10.1016/s0960-894x(00)00669-7
9871525 23683 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1cccc(I)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL125168 23683 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1cccc(I)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44461486 212142 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 564 15 3 9 3.7 CCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL79806 212142 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 564 15 3 9 3.7 CCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
9933039 169824 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1021/jm980521l
CHEMBL417613 169824 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1021/jm980521l
9915238 204945 2 None - 0 Human 8.2 pEC50 = 8.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1021/jm980521l
CHEMBL57486 204945 2 None - 0 Human 8.2 pEC50 = 8.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1021/jm980521l
137657762 166467 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 432 11 4 6 2.7 CCCS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C)n[nH]c3c2)c1 10.1021/acs.jmedchem.6b01197
CHEMBL4104183 166467 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 432 11 4 6 2.7 CCCS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C)n[nH]c3c2)c1 10.1021/acs.jmedchem.6b01197
9908924 148433 0 None 2 3 Human 7.2 pEC50 = 7.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm980521l
CHEMBL38538 148433 0 None 2 3 Human 7.2 pEC50 = 7.2 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm980521l
44461716 212091 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 605 17 3 8 5.4 CCCCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL79363 212091 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 605 17 3 8 5.4 CCCCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
45280021 129316 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 444 10 4 6 2.9 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CCC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.6b01197
CHEMBL3601307 129316 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 444 10 4 6 2.9 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CCC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.6b01197
44583033 192309 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900364m
CHEMBL486278 192309 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Binding affinity to beta3 adrenoceptorBinding affinity to beta3 adrenoceptor
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900364m
45380469 166537 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 432 10 4 6 2.7 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C(C)C)c3)ccc12 10.1021/acs.jmedchem.6b01197
CHEMBL4105097 166537 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 432 10 4 6 2.7 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C(C)C)c3)ccc12 10.1021/acs.jmedchem.6b01197
10184665 10763 51 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
4799 10763 51 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
7353 10763 51 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
CHEMBL1198857 10763 51 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
DB09082 10763 51 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
10076176 113212 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3126382 113212 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3139683 113212 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
44461717 112457 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 577 15 3 8 4.6 CCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
CHEMBL312546 112457 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro effective concentration against beta-3 adrenergic receptor.In vitro effective concentration against beta-3 adrenergic receptor.
ChEMBL 577 15 3 8 4.6 CCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(03)00491-8
1499 8872 47 None -588 17 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b01197
3779 8872 47 None -588 17 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b01197
536 8872 47 None -588 17 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b01197
CHEMBL434 8872 47 None -588 17 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b01197
DB01064 8872 47 None -588 17 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 minsAgonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b01197
10205362 123732 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 468 8 4 5 4.4 N#CN/C(=N\c1cc(Cl)cc(Cl)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL338618 123732 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro efficacy at human beta-3 adrenergic receptor.In vitro efficacy at human beta-3 adrenergic receptor.
ChEMBL 468 8 4 5 4.4 N#CN/C(=N\c1cc(Cl)cc(Cl)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44589400 201359 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
CHEMBL530556 201359 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
2303 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 9961 68 None -213 26 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
2662 18156 131 None 1 30 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
CHEMBL118 18156 131 None 1 30 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
2303 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 9961 68 None -213 26 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
28417 46813 49 None -2 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 46813 49 None -2 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
44589401 193526 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 475 8 1 5 4.3 OC(COc1ccc2c(c1)CCCN2Cc1ccccc1)CN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmc.2008.11.030
CHEMBL488793 193526 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 475 8 1 5 4.3 OC(COc1ccc2c(c1)CCCN2Cc1ccccc1)CN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmc.2008.11.030
2750 210840 76 None -7 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 210840 76 None -7 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
9904205 212629 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against Alpha-3A adrenergic receptorBinding affinity against Alpha-3A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 212629 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against Alpha-3A adrenergic receptorBinding affinity against Alpha-3A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
11758172 107711 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL293994 107711 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
6518171 175075 55 None -14 8 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 495 12 2 6 4.9 CN(CCOc1ccc(C[C@H](Nc2ccccc2C(=O)c2ccccc2)C(=O)O)cc1)c1ccccn1 nan
CHEMBL434063 175075 55 None -14 8 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 495 12 2 6 4.9 CN(CCOc1ccc(C[C@H](Nc2ccccc2C(=O)c2ccccc2)C(=O)O)cc1)c1ccccn1 nan
145990586 173622 0 None -23 11 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-CGP-12177 from human beta3-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta3-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 173622 0 None -23 11 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-CGP-12177 from human beta3-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta3-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
134551 7146 27 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 7146 27 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 7146 27 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 7146 27 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
3191 109635 97 None -20 25 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -20 25 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
1212 8443 50 None -630 65 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -630 65 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -630 65 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -630 65 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -630 65 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
10722793 120124 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL331744 120124 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
107715 207724 22 None -281 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -281 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -281 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
3914 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
39468 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
431 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
570 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
CHEMBL1201237 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
CHEMBL293030 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
DB01210 7527 35 None -45 7 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
64143 205643 62 None -1 8 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
CHEMBL584 205643 62 None -1 8 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
2585 7590 103 None -16 22 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -16 22 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -16 22 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -16 22 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -16 22 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
1752 52535 59 None -2 5 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
CHEMBL153062 52535 59 None -2 5 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
176 7186 66 None -10 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -10 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -10 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -10 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -10 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2291 9958 58 None -8 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 9958 58 None -8 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 9958 58 None -8 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 9958 58 None -8 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 9958 58 None -8 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2541 7573 120 None -4897 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
587 7573 120 None -4897 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
6907 7573 120 None -4897 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
CHEMBL1016 7573 120 None -4897 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
DB00796 7573 120 None -4897 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
DB13919 7573 120 None -4897 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
1836 9370 59 None -61 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 9370 59 None -61 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 9370 59 None -61 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 9370 59 None -61 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 9370 59 None -61 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
33624 10593 34 None -87 9 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
4061 10593 34 None -87 9 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
565 10593 34 None -87 9 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
CHEMBL499 10593 34 None -87 9 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
DB00373 10593 34 None -87 9 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
44112 128068 48 None -7 7 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 128068 48 None -7 7 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
3038500 16112 12 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL111201 16112 12 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
5353853 24758 47 None -25 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 24758 47 None -25 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 24758 47 None -25 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
127 9900 52 None -83 15 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
688095 9900 52 None -83 15 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL117405 9900 52 None -83 15 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
44190762 183659 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of radioligand from adrenergic beta3 receptorDisplacement of radioligand from adrenergic beta3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 183659 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of radioligand from adrenergic beta3 receptorDisplacement of radioligand from adrenergic beta3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
657255 205863 34 None -21 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 205863 34 None -21 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
46882804 12595 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human adrenergic beta3 receptorInhibition of human adrenergic beta3 receptor
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079045 12595 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human adrenergic beta3 receptorInhibition of human adrenergic beta3 receptor
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
4189 213701 96 None -28 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -28 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -28 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
42609939 192339 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 462 11 2 6 4.2 COc1ccc(CNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1OC 10.1016/j.bmc.2008.11.030
CHEMBL486327 192339 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 462 11 2 6 4.2 COc1ccc(CNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1OC 10.1016/j.bmc.2008.11.030
1548953 214458 27 None -19 17 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 214458 27 None -19 17 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
44589133 182623 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
CHEMBL458541 182623 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptorDisplacement of [125I]iodocyanopindolol from human adrenergic beta-3 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
3198 212292 76 None -31 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -31 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -31 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
2812 11551 101 None -35 34 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -35 34 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
1016 10519 78 None -33 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -33 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -33 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -33 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -33 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -33 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2247 7293 81 None -102 42 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -102 42 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -102 42 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -102 42 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -102 42 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
10381889 113846 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against Alpha-3A adrenergic receptorBinding affinity against Alpha-3A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 113846 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against Alpha-3A adrenergic receptorBinding affinity against Alpha-3A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
2176 9901 68 None -151 27 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
4828 9901 68 None -151 27 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
91 9901 68 None -151 27 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL500 9901 68 None -151 27 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
DB00960 9901 68 None -151 27 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
9873257 91720 16 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed in CHO cells by receptor binding assay
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22375 91720 16 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed in CHO cells by receptor binding assay
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
54757232 72290 0 None -123 3 Human 7.0 pKd = 7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830618 72290 0 None -123 3 Human 7.0 pKd = 7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54757026 72264 0 None -91 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830489 72264 0 None -91 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54756927 72261 0 None -301 3 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830486 72261 0 None -301 3 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
137 7158 52 None -74 12 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
2119 7158 52 None -74 12 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
563 7158 52 None -74 12 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
66368 7158 52 None -74 12 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
CHEMBL266195 7158 52 None -74 12 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
DB00866 7158 52 None -74 12 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
2176 9901 68 None -151 27 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
4828 9901 68 None -151 27 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
91 9901 68 None -151 27 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
CHEMBL500 9901 68 None -151 27 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
DB00960 9901 68 None -151 27 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
2303 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
4946 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
564 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
63 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
91536 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL27 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL452861 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
DB00571 9961 68 None -213 26 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
54757126 72267 0 None -109 3 Human 6.5 pKd = 6.5 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830492 72267 0 None -109 3 Human 6.5 pKd = 6.5 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54758320 72292 0 None -6 3 Human 6.5 pKd = 6.5 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830620 72292 0 None -6 3 Human 6.5 pKd = 6.5 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
54758415 72293 0 None -37 3 Human 6.4 pKd = 6.4 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830621 72293 0 None -37 3 Human 6.4 pKd = 6.4 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
54758417 72260 0 None -44 3 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830485 72260 0 None -44 3 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
54757229 72289 0 None -16 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830617 72289 0 None -16 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54756928 72262 0 None -28 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830487 72262 0 None -28 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
54757129 72268 0 None -23 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830493 72268 0 None -23 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54757027 72265 0 None -24 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830490 72265 0 None -24 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54669764 72266 0 None -218 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830491 72266 0 None -218 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
54757331 72291 0 None -77 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830619 72291 0 None -77 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54756929 72263 0 None -28 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830488 72263 0 None -28 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
24937389 24220 0 None 4 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 10 3 9 4.2 COCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257675 24220 0 None 4 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 10 3 9 4.2 COCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
44396798 176171 0 None 18 3 Human 9.0 pKi = 9.0 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL442225 176171 0 None 18 3 Human 9.0 pKi = 9.0 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
46889643 13422 0 None -37 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083368 13422 0 None -37 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2010.04.009
153287574 182026 0 None -13 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]-CGP12177 from human recombinant adrenergic Beta3 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from human recombinant adrenergic Beta3 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 182026 0 None -13 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]-CGP12177 from human recombinant adrenergic Beta3 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from human recombinant adrenergic Beta3 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
18662720 20101 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 477 9 4 7 2.1 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)N2CCCCC2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119210 20101 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 477 9 4 7 2.1 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)N2CCCCC2)cc1 10.1016/j.bmcl.2004.04.074
44423643 148834 0 None -3548 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL387852 148834 0 None -3548 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
24321330 13608 0 None -4 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 486 8 1 5 4.7 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083996 13608 0 None -4 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 486 8 1 5 4.7 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
46889770 13493 0 None -63 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 306 7 2 4 2.2 CC(C)c1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083670 13493 0 None -63 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 306 7 2 4 2.2 CC(C)c1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
52948792 24492 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258596 24492 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
44423646 92013 0 None -23 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL225775 92013 0 None -23 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
44333696 114121 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
CHEMBL317621 114121 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
44344670 120594 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 570 10 5 9 3.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc3sc(C)nc3c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL332529 120594 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 570 10 5 9 3.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc3sc(C)nc3c2)cc1 10.1016/j.bmcl.2004.04.074
52949488 24318 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258023 24318 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52943362 24320 0 None -2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 466 8 2 8 4.4 OC(CNC1CCN(c2ncnc3scc(-c4cccs4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258025 24320 0 None -2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 466 8 2 8 4.4 OC(CNC1CCN(c2ncnc3scc(-c4cccs4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
44333696 114121 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 486 11 4 7 3.4 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL317621 114121 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 486 11 4 7 3.4 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
10162297 160686 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL398322 160686 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
44334123 11841 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 350 8 4 5 1.6 CS(=O)(=O)Nc1cc(C(O)CNCCc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL105392 11841 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 350 8 4 5 1.6 CS(=O)(=O)Nc1cc(C(O)CNCCc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
18435434 101172 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 380 9 4 6 1.5 COc1ccc(CNCC(O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL250954 101172 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 380 9 4 6 1.5 COc1ccc(CNCC(O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
44444170 160683 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL398320 160683 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
44333828 11228 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 380 6 4 5 2.4 CS(=O)(=O)Nc1cc(C(O)CNC23CC4CC(CC(C4)C2)C3)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL101693 11228 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 380 6 4 5 2.4 CS(=O)(=O)Nc1cc(C(O)CNC23CC4CC(CC(C4)C2)C3)ccc1O 10.1016/s0960-894x(01)00628-x
46889767 13845 0 None -138 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 400 9 1 5 2.4 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085009 13845 0 None -138 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 400 9 1 5 2.4 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
44287321 107242 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 407 10 4 5 2.5 C[C@H](Cc1ccc(OC(C(=O)O)C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL290752 107242 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 407 10 4 5 2.5 C[C@H](Cc1ccc(OC(C(=O)O)C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
52947562 24459 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258486 24459 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
131801156 163934 14 None -51 5 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3
ChEMBL 417 5 2 6 4.4 O=C1CCc2cc(Nc3cc(OC4CCOCC4)c([N+](=O)[O-])cc3Cl)ccc2N1 10.6019/CHEMBL5212743
132486799 163934 14 None -51 5 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3
ChEMBL 417 5 2 6 4.4 O=C1CCc2cc(Nc3cc(OC4CCOCC4)c([N+](=O)[O-])cc3Cl)ccc2N1 10.6019/CHEMBL5212743
CHEMBL4075278 163934 14 None -51 5 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3
ChEMBL 417 5 2 6 4.4 O=C1CCc2cc(Nc3cc(OC4CCOCC4)c([N+](=O)[O-])cc3Cl)ccc2N1 10.6019/CHEMBL5212743
44344912 19922 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 528 11 6 8 2.4 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(CN)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119070 19922 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 528 11 6 8 2.4 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(CN)c2)cc1 10.1016/j.bmcl.2004.04.074
14823035 148341 2 None -354 3 Human 5.9 pKi = 5.9 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
CHEMBL38486 148341 2 None -354 3 Human 5.9 pKi = 5.9 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
4143663 13664 13 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(OC)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1084274 13664 13 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(OC)c1 10.1016/j.bmcl.2010.04.009
44444195 101311 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccc(Cl)cc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL251764 101311 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccc(Cl)cc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
18662696 11383 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 483 10 5 6 2.7 CNC(=O)c1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
CHEMBL102813 11383 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 483 10 5 6 2.7 CNC(=O)c1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
2662 18156 131 None 1 30 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
CHEMBL118 18156 131 None 1 30 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
2303 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 9961 68 None -213 26 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
44333737 11775 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 336 7 4 5 1.6 CS(=O)(=O)Nc1cc(C(O)CNCc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL105019 11775 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 336 7 4 5 1.6 CS(=O)(=O)Nc1cc(C(O)CNCc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
28417 46813 49 None -2 12 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 46813 49 None -2 12 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
19073121 10958 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 432 9 4 6 3.4 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccsc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL100138 10958 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 432 9 4 6 3.4 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccsc2)ccc1O 10.1016/s0960-894x(01)00629-1
52948728 24219 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257674 24219 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
19073196 114635 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 454 9 4 5 4.0 Cc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1C 10.1016/s0960-894x(01)00628-x
CHEMBL319257 114635 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 454 9 4 5 4.0 Cc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1C 10.1016/s0960-894x(01)00628-x
44444179 100917 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 508 10 4 5 4.5 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(Cl)c(Cl)c2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL249359 100917 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 508 10 4 5 4.5 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(Cl)c(Cl)c2)ccc1O 10.1016/j.bmcl.2007.05.030
2750 210840 76 None -7 12 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 210840 76 None -7 12 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
24937016 24529 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258706 24529 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
24936488 24421 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258373 24421 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
44344649 19988 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 591 12 5 8 4.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119120 19988 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 591 12 5 8 4.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.04.074
44396596 130078 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL361505 130078 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
52944986 24385 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
CHEMBL1258257 24385 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
71459884 85247 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 409 9 5 7 0.6 COc1ccc([C@@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(N)=O)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL2111776 85247 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 409 9 5 7 0.6 COc1ccc([C@@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(N)=O)cc1 10.1016/j.bmcl.2004.04.074
44344593 19335 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 11 5 8 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL118675 19335 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 11 5 8 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.04.074
155534733 178746 0 None 2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of beta-3 adrenergic receptor (unknown origin)Inhibition of beta-3 adrenergic receptor (unknown origin)
ChEMBL 269 3 3 8 -1.7 COC(=O)c1ncn([C@H]2[C@H](O)[C@H](O)[C@]3(CO)C[C@H]23)n1 10.1021/acs.jmedchem.8b01662
CHEMBL4470730 178746 0 None 2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of beta-3 adrenergic receptor (unknown origin)Inhibition of beta-3 adrenergic receptor (unknown origin)
ChEMBL 269 3 3 8 -1.7 COC(=O)c1ncn([C@H]2[C@H](O)[C@H](O)[C@]3(CO)C[C@H]23)n1 10.1021/acs.jmedchem.8b01662
122188571 129954 0 None -1318 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human adrenergic beta3 receptorDisplacement of [3H]CGP12177 from human adrenergic beta3 receptor
ChEMBL 486 5 4 9 1.8 CCCNc1nc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acs.jmedchem.7b00141
CHEMBL3612932 129954 0 None -1318 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human adrenergic beta3 receptorDisplacement of [3H]CGP12177 from human adrenergic beta3 receptor
ChEMBL 486 5 4 9 1.8 CCCNc1nc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acs.jmedchem.7b00141
44333890 11749 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 485 10 6 7 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C(=O)NO)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL104899 11749 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 485 10 6 7 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C(=O)NO)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
9958539 109882 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1021/jm990012z
CHEMBL307647 109882 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1021/jm990012z
24936489 24290 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257914 24290 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
5187268 13349 12 None -21 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 501 9 1 6 3.6 CC(C)c1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083053 13349 12 None -21 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 501 9 1 6 3.6 CC(C)c1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
46889730 13901 0 None -87 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 436 8 1 5 3.6 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085270 13901 0 None -87 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 436 8 1 5 3.6 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
52941603 24071 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 573 9 2 9 3.8 O=C(c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1)N1CCOCC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257204 24071 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 573 9 2 9 3.8 O=C(c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1)N1CCOCC1 10.1016/j.bmcl.2010.08.039
44333757 11355 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 487 11 4 8 2.8 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c(OC)n1 10.1016/s0960-894x(01)00629-1
CHEMBL102611 11355 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 487 11 4 8 2.8 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c(OC)n1 10.1016/s0960-894x(01)00629-1
10207209 176005 0 None 5 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL440961 176005 0 None 5 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
44333818 11514 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 440 10 4 5 3.2 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)Cc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL103743 11514 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 440 10 4 5 3.2 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)Cc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
44444159 101245 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 288 6 4 6 -0.3 CS(=O)(=O)Nc1cc(C(=O)C[C@@H](O)CN)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL251363 101245 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 288 6 4 6 -0.3 CS(=O)(=O)Nc1cc(C(=O)C[C@@H](O)CN)ccc1O 10.1016/j.bmcl.2007.05.030
52949934 24420 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 398 7 2 7 3.0 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258372 24420 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 398 7 2 7 3.0 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
46889727 13421 0 None -19 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(OC)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083366 13421 0 None -19 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(OC)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
44333719 114279 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 366 8 4 6 1.6 COc1ccc(CNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL318579 114279 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 366 8 4 6 1.6 COc1ccc(CNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
9872113 115560 11 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 544 12 4 7 4.4 CS(=O)(=O)Nc1cc([C@@H](O)CNC(c2ccc(OC(F)F)cc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL320915 115560 11 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 544 12 4 7 4.4 CS(=O)(=O)Nc1cc([C@@H](O)CNC(c2ccc(OC(F)F)cc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00628-x
44444168 101249 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 514 13 4 7 3.6 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)CCc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL251370 101249 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 514 13 4 7 3.6 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)CCc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
19073202 11789 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 463 13 5 6 2.3 CNC(=O)CCCCC(Cc1ccccc1)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
CHEMBL105095 11789 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 463 13 5 6 2.3 CNC(=O)CCCCC(Cc1ccccc1)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
6518171 175075 55 None -14 8 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 495 12 2 6 4.9 CN(CCOc1ccc(C[C@H](Nc2ccccc2C(=O)c2ccccc2)C(=O)O)cc1)c1ccccn1 nan
CHEMBL434063 175075 55 None -14 8 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 495 12 2 6 4.9 CN(CCOc1ccc(C[C@H](Nc2ccccc2C(=O)c2ccccc2)C(=O)O)cc1)c1ccccn1 nan
44344829 16890 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 533 10 5 7 3.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL115628 16890 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 533 10 5 7 3.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
44344592 175102 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 11 5 8 3.0 COc1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL434223 175102 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 11 5 8 3.0 COc1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.04.074
44396568 74060 0 None 9 3 Human 7.8 pKi = 7.8 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL188196 74060 0 None 9 3 Human 7.8 pKi = 7.8 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
24885648 23908 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 460 8 2 7 4.4 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1255596 23908 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 460 8 2 7 4.4 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
52947443 24386 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(F)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258258 24386 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(F)c1 10.1016/j.bmcl.2010.08.039
44444184 173652 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 574 15 4 9 3.1 COc1ccc(CC(Cc2ccc(OC)c(OC)c2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL428584 173652 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 574 15 4 9 3.1 COc1ccc(CC(Cc2ccc(OC)c(OC)c2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
44435200 156454 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Antagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assay
ChEMBL 345 4 0 2 5.8 O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL394755 156454 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Antagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assay
ChEMBL 345 4 0 2 5.8 O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
44444158 101244 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 490 10 4 7 3.3 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2F)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251362 101244 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 490 10 4 7 3.3 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2F)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2007.05.030
9837752 114959 3 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 246 4 4 5 -0.2 CS(=O)(=O)Nc1cc(C(O)CN)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL319632 114959 3 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 246 4 4 5 -0.2 CS(=O)(=O)Nc1cc(C(O)CN)ccc1O 10.1016/s0960-894x(01)00628-x
12047933 161644 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 246 4 4 5 -0.2 CS(=O)(=O)Nc1cc([C@@H](O)CN)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL400645 161644 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 246 4 4 5 -0.2 CS(=O)(=O)Nc1cc([C@@H](O)CN)ccc1O 10.1016/j.bmcl.2007.05.030
4080436 13491 3 None -1479 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 279 6 1 4 1.9 CC(C)c1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083668 13491 3 None -1479 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 279 6 1 4 1.9 CC(C)c1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
44345049 103185 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 543 11 6 8 2.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(C(=O)O)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL261933 103185 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 543 11 6 8 2.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(C(=O)O)c2)cc1 10.1016/j.bmcl.2004.04.074
1499 8872 47 None -588 17 Human 4.7 pKi = 4.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
3779 8872 47 None -588 17 Human 4.7 pKi = 4.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
536 8872 47 None -588 17 Human 4.7 pKi = 4.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
CHEMBL434 8872 47 None -588 17 Human 4.7 pKi = 4.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
DB01064 8872 47 None -588 17 Human 4.7 pKi = 4.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
134551 7146 27 None -79 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 7146 27 None -79 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 7146 27 None -79 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 7146 27 None -79 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
44287268 165796 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 441 11 3 5 4.5 CC(C)OP(=O)(O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
CHEMBL40966 165796 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 441 11 3 5 4.5 CC(C)OP(=O)(O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
44344650 20532 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 577 10 5 7 3.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(Br)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119533 20532 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 577 10 5 7 3.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(Br)c2)cc1 10.1016/j.bmcl.2004.04.074
10231679 101090 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 572 14 4 7 4.4 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL250553 101090 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 572 14 4 7 4.4 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
44344713 17013 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 535 11 5 7 3.5 C[C@@](NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(C(=O)Nc1ccccc1)c1ccc(OC(F)F)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL116080 17013 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 535 11 5 7 3.5 C[C@@](NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(C(=O)Nc1ccccc1)c1ccc(OC(F)F)cc1 10.1016/j.bmcl.2004.04.074
3191 109635 97 None -20 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -20 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
44287337 157937 0 None -17 3 Human 5.7 pKi = 5.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 378 9 4 5 2.5 C[C@H](Cc1ccc(OCC(=O)NO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL39596 157937 0 None -17 3 Human 5.7 pKi = 5.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 378 9 4 5 2.5 C[C@H](Cc1ccc(OCC(=O)NO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44286980 154671 0 None 3 2 Human 4.7 pKi = 4.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 397 9 3 4 3.8 C[C@H](Cc1ccc(OCP(C)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL39334 154671 0 None 3 2 Human 4.7 pKi = 4.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 397 9 3 4 3.8 C[C@H](Cc1ccc(OCP(C)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44333968 11912 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 542 11 4 6 5.1 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c3ccccc23)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL105758 11912 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 542 11 4 6 5.1 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c3ccccc23)ccc1O 10.1016/s0960-894x(01)00629-1
44396729 73636 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(N)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL186247 73636 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(N)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44333932 11292 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 10 4 7 3.4 COc1ccc(C(C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL102222 11292 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 10 4 7 3.4 COc1ccc(C(C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/s0960-894x(01)00628-x
44344656 118109 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 584 13 6 8 3.1 CCCNC(=O)c1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL326820 118109 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 584 13 6 8 3.1 CCCNC(=O)c1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.04.074
44444157 175668 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 412 8 4 6 2.5 COc1ccc(C(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2F)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL438343 175668 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 412 8 4 6 2.5 COc1ccc(C(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2F)cc1 10.1016/j.bmcl.2007.05.030
146015362 7734 10 None -8 3 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
3462 7734 10 None -8 3 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
5486546 7734 10 None -8 3 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
CHEMBL1204876 7734 10 None -8 3 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its binding affinity to CHO cells expressing the cloned human Beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
9870286 116484 10 None 190 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 492 11 4 6 4.0 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL322862 116484 10 None 190 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 492 11 4 6 4.0 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
9870286 116484 10 None 190 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 492 11 4 6 4.0 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL322862 116484 10 None 190 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 492 11 4 6 4.0 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
9871887 109977 0 None -10 4 Human 7.7 pKi = 7.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm990012z
CHEMBL308351 109977 0 None -10 4 Human 7.7 pKi = 7.7 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm990012z
44333524 11426 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 510 10 4 6 4.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(OC(F)(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL103117 11426 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 510 10 4 6 4.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(OC(F)(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
44334231 11607 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 451 9 4 6 3.2 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C#N)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL104217 11607 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 451 9 4 6 3.2 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C#N)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
44286965 167188 0 None -8 3 Human 5.7 pKi = 5.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 349 9 3 4 3.0 C[C@H](Cc1ccc(OCCO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL41113 167188 0 None -8 3 Human 5.7 pKi = 5.7 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 349 9 3 4 3.0 C[C@H](Cc1ccc(OCCO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44423644 92184 0 None -269 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL226348 92184 0 None -269 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
44333605 11374 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 515 11 5 8 1.8 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)(C(N)=O)c2ccc(OC)cc2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL102759 11374 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 515 11 5 8 1.8 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)(C(N)=O)c2ccc(OC)cc2)cc1 10.1016/s0960-894x(01)00628-x
44344758 20001 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 513 10 5 7 3.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2C)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119128 20001 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 513 10 5 7 3.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2C)cc1 10.1016/j.bmcl.2004.04.074
46889701 13849 0 None -16 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 500 9 2 6 4.0 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(O)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085014 13849 0 None -16 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 500 9 2 6 4.0 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(O)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
44423640 148833 0 None -1584 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 398 9 3 6 2.2 C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cc(Br)no1 10.1016/j.bmc.2007.01.056
CHEMBL387851 148833 0 None -1584 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 398 9 3 6 2.2 C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cc(Br)no1 10.1016/j.bmc.2007.01.056
1212 8443 50 None -630 65 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -630 65 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -630 65 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -630 65 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -630 65 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
46889670 13784 0 None -74 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 533 7 2 5 5.2 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084772 13784 0 None -74 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 533 7 2 5 5.2 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
44344671 17184 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 515 10 6 8 2.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(O)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL116294 17184 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 515 10 6 8 2.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(O)cc2)cc1 10.1016/j.bmcl.2004.04.074
52948056 24291 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257915 24291 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
19073276 11523 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 456 10 4 6 3.4 COc1cccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/s0960-894x(01)00628-x
CHEMBL103784 11523 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 456 10 4 6 3.4 COc1cccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/s0960-894x(01)00628-x
44333796 114192 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 482 9 4 6 4.6 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc3sccc3c2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL318074 114192 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 482 9 4 6 4.6 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc3sccc3c2)ccc1O 10.1016/s0960-894x(01)00629-1
46889852 13304 0 None -1148 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 428 7 2 4 4.7 O=C(c1ccccc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1082827 13304 0 None -1148 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 428 7 2 4 4.7 O=C(c1ccccc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
46889810 14188 0 None -457 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 414 7 2 3 5.0 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086542 14188 0 None -457 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 414 7 2 3 5.0 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2010.04.009
46889699 13420 0 None -58 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 470 8 1 5 4.1 C=CCc1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083364 13420 0 None -58 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 470 8 1 5 4.1 C=CCc1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
145973771 171498 0 None -2 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-CGP12177 from human adrenergic beta-3 receptor expressed in HEK Flp-In cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-CGP12177 from human adrenergic beta-3 receptor expressed in HEK Flp-In cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 171498 0 None -2 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-CGP12177 from human adrenergic beta-3 receptor expressed in HEK Flp-In cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-CGP12177 from human adrenergic beta-3 receptor expressed in HEK Flp-In cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
44344870 18469 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 567 10 5 7 4.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL118121 18469 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 567 10 5 7 4.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
10119452 174196 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 12 4 7 3.9 COc1ccc([C@@H](Cc2ccc(Cl)cc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL429665 174196 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 12 4 7 3.9 COc1ccc([C@@H](Cc2ccc(Cl)cc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
44333864 115477 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 433 9 4 7 2.8 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2nccs2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL320818 115477 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 433 9 4 7 2.8 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2nccs2)ccc1O 10.1016/s0960-894x(01)00629-1
107715 207724 22 None -281 20 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -281 20 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -281 20 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
44423645 92185 0 None -158 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL226349 92185 0 None -158 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 3 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
44333758 11347 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 457 10 4 7 2.8 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cn1 10.1016/s0960-894x(01)00629-1
CHEMBL102580 11347 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 457 10 4 7 2.8 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cn1 10.1016/s0960-894x(01)00629-1
10117815 100757 0 None 60 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL248548 100757 0 None 60 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
46889854 14080 0 None -831 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086077 14080 0 None -831 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
44435193 98000 0 None -14 7 Human 5.6 pKi = 5.6 Binding
Antagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL240045 98000 0 None -14 7 Human 5.6 pKi = 5.6 Binding
Antagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic beta3 receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
3914 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
39468 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
431 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
570 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
CHEMBL1201237 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
CHEMBL293030 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
DB01210 7527 35 None -45 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O nan
64143 205643 62 None -1 8 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
CHEMBL584 205643 62 None -1 8 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
44333531 114173 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 506 10 4 6 4.5 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccccc12 10.1016/s0960-894x(01)00629-1
CHEMBL317920 114173 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 506 10 4 6 4.5 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccccc12 10.1016/s0960-894x(01)00629-1
44344909 170085 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 586 14 5 9 2.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(OCCN(C)C)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL418867 170085 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 586 14 5 9 2.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(OCCN(C)C)cc2)cc1 10.1016/j.bmcl.2004.04.074
52948612 24102 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.1 O=C(O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257323 24102 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.1 O=C(O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
44444156 101243 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 510 11 4 6 4.1 CS(=O)(=O)Nc1c(O)ccc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)c1F 10.1016/j.bmcl.2007.05.030
CHEMBL251361 101243 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 510 11 4 6 4.1 CS(=O)(=O)Nc1c(O)ccc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)c1F 10.1016/j.bmcl.2007.05.030
44344806 20874 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 513 10 5 7 3.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(C)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119786 20874 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 513 10 5 7 3.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(C)cc2)cc1 10.1016/j.bmcl.2004.04.074
18662716 121220 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 10 5 9 2.5 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL333334 121220 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 10 5 9 2.5 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.04.074
44333764 11333 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 448 8 4 5 3.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC(c2ccc(F)cc2)c2ccc(F)cc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL102471 11333 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 448 8 4 5 3.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC(c2ccc(F)cc2)c2ccc(F)cc2)ccc1O 10.1016/s0960-894x(01)00628-x
44444193 160594 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2cccc(Cl)c2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL398241 160594 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2cccc(Cl)c2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
24937140 24456 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258483 24456 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
46889768 13847 0 None -323 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 402 8 1 5 2.8 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085010 13847 0 None -323 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 402 8 1 5 2.8 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
44344757 18726 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 409 9 5 7 0.6 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(N)=O)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL118287 18726 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 409 9 5 7 0.6 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(N)=O)cc1 10.1016/j.bmcl.2004.04.074
44444163 101180 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 528 13 4 8 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)CC(=O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL250978 101180 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 528 13 4 8 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)CC(=O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
2585 7590 103 None -16 22 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -16 22 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -16 22 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -16 22 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -16 22 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
44396532 73530 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185836 73530 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
24937013 24221 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257676 24221 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
44333551 116485 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 526 10 6 7 3.1 CC(=O)Nc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(NC(C)=O)cc2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL322863 116485 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 526 10 6 7 3.1 CC(=O)Nc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(NC(C)=O)cc2)cc1 10.1016/s0960-894x(01)00628-x
24936763 24388 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.9 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258260 24388 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.9 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
18662700 85246 0 None - 1 Human 4.5 pKi = 4.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL2111775 85246 0 None - 1 Human 4.5 pKi = 4.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
145990586 173622 0 None -23 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to andrenergic beta3 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic beta3 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 173622 0 None -23 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to andrenergic beta3 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic beta3 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
44444187 101242 0 None 9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251347 101242 0 None 9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
18662712 20924 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 499 11 5 7 2.5 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)NCc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119831 20924 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 499 11 5 7 2.5 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)NCc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
44344578 117431 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 11 5 8 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2OC)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL325853 117431 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 11 5 8 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2OC)cc1 10.1016/j.bmcl.2004.04.074
2770390 13494 10 None -20 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 499 10 1 6 3.2 C=CCc1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083672 13494 10 None -20 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 499 10 1 6 3.2 C=CCc1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
1752 52535 59 None -2 5 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
CHEMBL153062 52535 59 None -2 5 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
176 7186 66 None -10 31 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -10 31 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -10 31 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -10 31 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -10 31 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2291 9958 58 None -8 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 9958 58 None -8 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 9958 58 None -8 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 9958 58 None -8 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 9958 58 None -8 12 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
44334164 11205 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 420 12 4 5 3.6 CCCCCC(Cc1ccccc1)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
CHEMBL101591 11205 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 420 12 4 5 3.6 CCCCCC(Cc1ccccc1)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
44333734 12015 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc([C@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
CHEMBL106329 12015 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc([C@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
2541 7573 120 None -4897 6 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
587 7573 120 None -4897 6 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
6907 7573 120 None -4897 6 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
CHEMBL1016 7573 120 None -4897 6 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
DB00796 7573 120 None -4897 6 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
DB13919 7573 120 None -4897 6 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O nan
1836 9370 59 None -61 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 9370 59 None -61 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 9370 59 None -61 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 9370 59 None -61 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 9370 59 None -61 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL4566600 220793 0 None -1 6 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl ADRB3
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5212743
CHEMBL4745071 220793 0 None -1 6 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl ADRB3
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5212743
9957065 11396 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
CHEMBL102891 11396 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
18662716 121220 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 10 5 9 2.5 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL333334 121220 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 529 10 5 9 2.5 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.04.074
44396659 74138 0 None 6 3 Human 7.5 pKi = 7.5 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188622 74138 0 None 6 3 Human 7.5 pKi = 7.5 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
44334131 11845 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 438 11 4 8 1.2 COC(=O)COc1ccc(CCNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL105430 11845 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 438 11 4 8 1.2 COC(=O)COc1ccc(CCNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
52947431 24141 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 7 1 7 4.4 OC(COc1ccccc1)CN1CCCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257440 24141 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 7 1 7 4.4 OC(COc1ccccc1)CN1CCCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
18662710 20548 0 None - 1 Human 4.5 pKi = 4.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 499 10 4 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)N(C)c2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119539 20548 0 None - 1 Human 4.5 pKi = 4.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 499 10 4 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)N(C)c2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
52946430 24597 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 517 9 3 8 3.7 CNC(=O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258940 24597 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 517 9 3 8 3.7 CNC(=O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
4276762 13726 10 None -11 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 530 8 1 6 4.9 COc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(C(C)(C)C)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1084526 13726 10 None -11 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 530 8 1 6 4.9 COc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(C(C)(C)C)c1 10.1016/j.bmcl.2010.04.009
33624 10593 34 None -87 9 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
4061 10593 34 None -87 9 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
565 10593 34 None -87 9 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
CHEMBL499 10593 34 None -87 9 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
DB00373 10593 34 None -87 9 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
44344674 20940 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 515 10 6 8 2.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(O)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119860 20940 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 515 10 6 8 2.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(O)c2)cc1 10.1016/j.bmcl.2004.04.074
44444181 161506 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 558 13 4 7 4.2 CS(=O)(=O)Nc1cc(C[C@H](O)CNC(c2ccc(OC(F)F)cc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL399867 161506 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 558 13 4 7 4.2 CS(=O)(=O)Nc1cc(C[C@H](O)CNC(c2ccc(OC(F)F)cc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
46889729 13850 0 None -67 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 434 9 1 5 3.2 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085016 13850 0 None -67 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 434 9 1 5 3.2 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
44112 128068 48 None -7 7 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 128068 48 None -7 7 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
24936625 24256 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257798 24256 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
15221053 211375 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 364 11 3 6 2.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL73220 211375 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 364 11 3 6 2.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
5353853 24758 47 None -25 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 24758 47 None -25 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 24758 47 None -25 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
127 9900 52 None -83 15 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
688095 9900 52 None -83 15 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL117405 9900 52 None -83 15 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
19073158 11295 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 426 9 4 5 3.4 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL102257 11295 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 426 9 4 5 3.4 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
19073158 11295 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 426 9 4 5 3.4 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccccc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL102257 11295 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 426 9 4 5 3.4 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccccc2)ccc1O 10.1016/s0960-894x(01)00629-1
44444160 161647 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 408 10 4 7 1.5 COc1ccc(CNC[C@H](O)CC(=O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL400669 161647 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 408 10 4 7 1.5 COc1ccc(CNC[C@H](O)CC(=O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
44312269 211218 0 None -5 3 Human 4.4 pKi = 4.4 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 382 10 3 5 3.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
CHEMBL72168 211218 0 None -5 3 Human 4.4 pKi = 4.4 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 382 10 3 5 3.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
52943968 24566 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258824 24566 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
18662711 17808 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL117577 17808 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
44344911 19593 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 589 13 5 10 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL118834 19593 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 589 13 5 10 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmcl.2004.04.074
44345040 119626 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 573 13 6 9 2.4 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(OCC(=O)O)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL330924 119626 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 573 13 6 9 2.4 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(OCC(=O)O)cc2)cc1 10.1016/j.bmcl.2004.04.074
52948613 24104 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.8 OC(COc1ccccc1)CN1CCC(Nc2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257325 24104 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.8 OC(COc1ccccc1)CN1CCC(Nc2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
44286983 148488 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 362 9 3 4 2.5 C[C@H](Cc1ccc(OCC(N)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL38569 148488 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 362 9 3 4 2.5 C[C@H](Cc1ccc(OCC(N)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44333761 11300 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 316 7 4 5 1.6 CCC(C)(C)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
CHEMBL102291 11300 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 316 7 4 5 1.6 CCC(C)(C)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
44444164 101212 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 394 10 4 6 1.9 COc1ccc(CNC[C@H](O)CCc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251175 101212 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 394 10 4 6 1.9 COc1ccc(CNC[C@H](O)CCc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
65772 67177 8 None -204 6 Human 5.4 pKi = 5.4 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm990012z
CHEMBL174984 67177 8 None -204 6 Human 5.4 pKi = 5.4 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm990012z
657255 205863 34 None -21 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 205863 34 None -21 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
2796082 13607 4 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1083995 13607 4 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
44333651 115001 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 558 13 4 7 4.6 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL319687 115001 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 558 13 4 7 4.6 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/s0960-894x(01)00629-1
44344787 16859 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 533 10 5 7 3.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2Cl)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL115424 16859 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 533 10 5 7 3.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2Cl)cc1 10.1016/j.bmcl.2004.04.074
46889700 13848 0 None -295 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 472 7 1 5 4.5 CC(C)c1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085013 13848 0 None -295 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 472 7 1 5 4.5 CC(C)c1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL4445645 220713 18 None -4 5 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of Beta3GPCRScan assay: inhibition of Beta3
ChEMBL None None None C[C@@H]1CN(c2ncc(Cl)c(Nc3ccc4c(c3)n(CCC(C)(C)O)c(=O)n4C)n2)C[C@H](C)C1(F)F 10.6019/CHEMBL5058646
44312421 170117 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 392 13 3 6 2.9 C[C@H](Cc1ncc(CCCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL419085 170117 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 392 13 3 6 2.9 C[C@H](Cc1ncc(CCCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
44444188 101270 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1cccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL251554 101270 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1cccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL4445645 220713 18 None -4 5 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of Beta3GPCRScan assay: inhibition of Beta3
ChEMBL None None None C[C@@H]1CN(c2ncc(Cl)c(Nc3ccc4c(c3)n(CCC(C)(C)O)c(=O)n4C)n2)C[C@H](C)C1(F)F 10.6019/CHEMBL5058646
11432806 72971 0 None 12 3 Human 8.4 pKi = 8.4 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
11432806 72971 0 None 12 3 Human 8.4 pKi = 8.4 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL184407 72971 0 None 12 3 Human 8.4 pKi = 8.4 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL184407 72971 0 None 12 3 Human 8.4 pKi = 8.4 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-3 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44344714 16967 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 512 10 6 7 2.0 C[C@@](NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(C(=O)Nc1ccccc1)c1ccc(C(N)=O)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL115972 16967 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 512 10 6 7 2.0 C[C@@](NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(C(=O)Nc1ccccc1)c1ccc(C(N)=O)cc1 10.1016/j.bmcl.2004.04.074
9870286 116484 10 None -190 2 Mouse 5.4 pKi = 5.4 Binding
Tested for binding affinity to murine Beta-3 adrenergic receptorTested for binding affinity to murine Beta-3 adrenergic receptor
ChEMBL 492 11 4 6 4.0 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL322862 116484 10 None -190 2 Mouse 5.4 pKi = 5.4 Binding
Tested for binding affinity to murine Beta-3 adrenergic receptorTested for binding affinity to murine Beta-3 adrenergic receptor
ChEMBL 492 11 4 6 4.0 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
4421983 14051 5 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 484 9 1 5 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086005 14051 5 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 484 9 1 5 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
52946537 24495 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258599 24495 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
46889772 13767 0 None -4073 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 563 8 2 6 5.2 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC1)C2=O 10.1016/j.bmcl.2010.04.009
CHEMBL1084707 13767 0 None -4073 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 563 8 2 6 5.2 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC1)C2=O 10.1016/j.bmcl.2010.04.009
26162 109859 14 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 288 6 4 5 0.8 CC(C)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
CHEMBL30746 109859 14 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 288 6 4 5 0.8 CC(C)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
3687256 13606 7 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 500 8 1 5 5.0 Cc1ccc(C(C)C)c(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1083994 13606 7 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 500 8 1 5 5.0 Cc1ccc(C(C)C)c(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
4189 213701 96 None -28 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -28 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -28 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
19073116 116181 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 494 9 4 5 4.7 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc(Cl)c(Cl)c2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL321987 116181 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 494 9 4 5 4.7 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc(Cl)c(Cl)c2)ccc1O 10.1016/s0960-894x(01)00628-x
52949489 24319 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258024 24319 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
1548953 214458 27 None -19 17 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 214458 27 None -19 17 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
44333846 174727 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 476 9 4 5 4.5 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2cccc3ccccc23)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL431638 174727 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 476 9 4 5 4.5 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2cccc3ccccc23)ccc1O 10.1016/s0960-894x(01)00629-1
44333716 114161 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 432 9 4 5 3.6 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)C2CCCCC2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL317852 114161 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 432 9 4 5 3.6 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)C2CCCCC2)ccc1O 10.1016/s0960-894x(01)00628-x
19073138 11402 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 456 10 4 6 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL102928 11402 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 456 10 4 6 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
19073138 11402 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 456 10 4 6 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
CHEMBL102928 11402 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 456 10 4 6 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
44344960 17277 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 456 10 4 6 3.4 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL116715 17277 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 456 10 4 6 3.4 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2004.04.074
19073145 11427 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 504 10 4 7 2.8 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc(S(C)(=O)=O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL103118 11427 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 504 10 4 7 2.8 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc(S(C)(=O)=O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
44345048 118075 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 573 13 6 9 2.4 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(OCC(=O)O)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL326612 118075 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 573 13 6 9 2.4 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(OCC(=O)O)c2)cc1 10.1016/j.bmcl.2004.04.074
46889811 13227 0 None -2290 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 444 8 2 4 5.0 COc1ccc(CC2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1082500 13227 0 None -2290 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 444 8 2 4 5.0 COc1ccc(CC2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
44344819 120770 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 559 12 5 9 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(OC)c(OC)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL332632 120770 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 559 12 5 9 3.0 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(OC)c(OC)c2)cc1 10.1016/j.bmcl.2004.04.074
2796082 13607 4 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1083995 13607 4 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
10227108 101279 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251580 101279 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
3198 212292 76 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
44344828 16889 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 551 10 5 7 3.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)cc2F)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL115627 16889 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 551 10 5 7 3.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)cc2F)cc1 10.1016/j.bmcl.2004.04.074
52943932 24528 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 485 8 2 8 4.2 N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258705 24528 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 485 8 2 8 4.2 N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
44333923 11339 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 380 9 4 6 1.6 COc1ccc(CCNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL102522 11339 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 380 9 4 6 1.6 COc1ccc(CCNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00628-x
19073210 11441 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 436 13 5 6 2.6 CS(=O)(=O)Nc1cc(C(O)CNC(CCCCCO)Cc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL103219 11441 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 436 13 5 6 2.6 CS(=O)(=O)Nc1cc(C(O)CNC(CCCCCO)Cc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
24937269 24419 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258371 24419 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
44344575 17811 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 591 12 5 8 4.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL117596 17811 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 591 12 5 8 4.7 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2004.04.074
44333797 11425 0 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 424 11 5 7 1.1 CS(=O)(=O)Nc1cc(C(O)CNCCc2ccc(OCC(=O)O)cc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL103096 11425 0 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 424 11 5 7 1.1 CS(=O)(=O)Nc1cc(C(O)CNCCc2ccc(OCC(=O)O)cc2)ccc1O 10.1016/s0960-894x(01)00628-x
2769774 13490 17 None -707 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 277 7 1 4 1.5 C=CCc1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083667 13490 17 None -707 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 277 7 1 4 1.5 C=CCc1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
24937390 24387 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 8 3 8 4.4 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258259 24387 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 490 8 3 8 4.4 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
44444162 161735 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 13 4 7 3.9 CS(=O)(=O)Nc1cc(C(=O)C[C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL401135 161735 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 13 4 7 3.9 CS(=O)(=O)Nc1cc(C(=O)C[C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
44344820 121288 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 601 10 5 7 4.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cc(Cl)c(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL333551 121288 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 601 10 5 7 4.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cc(Cl)c(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
33630 185736 99 None -10 28 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assayDisplacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 185736 99 None -10 28 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assayDisplacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
19073142 162521 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 482 11 4 5 4.5 CCc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1CC 10.1016/s0960-894x(01)00628-x
CHEMBL405622 162521 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 482 11 4 5 4.5 CCc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1CC 10.1016/s0960-894x(01)00628-x
44344910 119677 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 586 14 5 9 2.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(OCCN(C)C)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL331027 119677 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 586 14 5 9 2.9 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(OCCN(C)C)c2)cc1 10.1016/j.bmcl.2004.04.074
164451 109954 14 None -1 3 Human 6.3 pKi = 6.3 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 361 12 3 6 1.6 O=C(O)COc1ccc(OCCNC[C@H](O)COc2ccccc2)cc1 10.1016/0960-894X(96)00417-9
CHEMBL308150 109954 14 None -1 3 Human 6.3 pKi = 6.3 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 361 12 3 6 1.6 O=C(O)COc1ccc(OCCNC[C@H](O)COc2ccccc2)cc1 10.1016/0960-894X(96)00417-9
10140092 101280 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251581 101280 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
2812 11551 101 None -35 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -35 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44333738 113971 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 410 10 4 7 1.6 COc1ccc(CCNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
CHEMBL316546 113971 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 410 10 4 7 1.6 COc1ccc(CCNCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/s0960-894x(01)00628-x
44286964 170175 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 4 4 3.1 C[C@H](Cc1ccc(OCP(=O)(O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL41948 170175 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 4 4 3.1 C[C@H](Cc1ccc(OCP(=O)(O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44333795 11313 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 464 13 4 7 2.7 COC(=O)CCCCC(Cc1ccccc1)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
CHEMBL102364 11313 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 464 13 4 7 2.7 COC(=O)CCCCC(Cc1ccccc1)NCC(O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1016/s0960-894x(01)00628-x
1016 10519 78 None -33 35 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -33 35 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -33 35 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -33 35 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -33 35 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -33 35 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44333733 11879 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 412 8 4 5 3.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC(c2ccccc2)c2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL105603 11879 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 412 8 4 5 3.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC(c2ccccc2)c2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
52943383 24353 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 544 9 2 8 5.3 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258142 24353 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 544 9 2 8 5.3 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2010.08.039
44444189 101271 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 586 15 4 7 4.8 CS(=O)(=O)Nc1cc(C[C@@H](O)CN[C@@H](CCc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL251555 101271 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 586 15 4 7 4.8 CS(=O)(=O)Nc1cc(C[C@@H](O)CN[C@@H](CCc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
46889771 13766 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084706 13766 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
10230413 101140 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 12 4 7 3.9 COc1ccc([C@@H](Cc2cccc(Cl)c2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL250755 101140 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 12 4 7 3.9 COc1ccc([C@@H](Cc2cccc(Cl)c2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
9960584 161408 0 None 10 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL399329 161408 0 None 10 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
24937137 24530 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258707 24530 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
2247 7293 81 None -102 42 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -102 42 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -102 42 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -102 42 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -102 42 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
44344618 16876 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 513 10 5 7 3.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(C)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL115538 16876 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 513 10 5 7 3.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cccc(C)c2)cc1 10.1016/j.bmcl.2004.04.074
24936882 24354 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 512 9 4 10 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258143 24354 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 512 9 4 10 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
24936883 24103 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257324 24103 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
46889769 13492 0 None -2570 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 304 8 2 4 1.8 C=CCc1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083669 13492 0 None -2570 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 304 8 2 4 1.8 C=CCc1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
52941476 24457 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258484 24457 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
52948805 24527 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 502 9 2 7 5.5 CC(C)c1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258704 24527 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 502 9 2 7 5.5 CC(C)c1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
2176 9901 68 None -151 27 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
4828 9901 68 None -151 27 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
91 9901 68 None -151 27 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL500 9901 68 None -151 27 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
DB00960 9901 68 None -151 27 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
567 7512 16 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
9841972 7512 16 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
CHEMBL284782 7512 16 None -1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(01)00628-x
52946357 24494 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258598 24494 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
10544781 211464 0 None -109 3 Human 4.2 pKi = 4.2 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 335 5 2 7 2.2 COc1cc(CC2NCCc3nc(N)sc32)cc(OC)c1OC 10.1021/jm990012z
CHEMBL73917 211464 0 None -109 3 Human 4.2 pKi = 4.2 Binding
Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 335 5 2 7 2.2 COc1cc(CC2NCCc3nc(N)sc32)cc(OC)c1OC 10.1021/jm990012z
44333847 11751 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 506 11 4 6 4.3 Cc1cc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1OC(F)F 10.1016/s0960-894x(01)00629-1
CHEMBL104905 11751 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 506 11 4 6 4.3 Cc1cc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1OC(F)F 10.1016/s0960-894x(01)00629-1
46889728 13489 0 None -18 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 516 9 1 6 4.7 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3ccccc3C(C)C)CC1)C2=O 10.1016/j.bmcl.2010.04.009
CHEMBL1083666 13489 0 None -18 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 516 9 1 6 4.7 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3ccccc3C(C)C)CC1)C2=O 10.1016/j.bmcl.2010.04.009
44444149 101035 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 394 8 4 6 2.3 COc1ccc(C(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL250191 101035 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 394 8 4 6 2.3 COc1ccc(C(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
10186965 175579 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 12 4 7 3.9 COc1ccc([C@@H](Cc2ccccc2Cl)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL437578 175579 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 534 12 4 7 3.9 COc1ccc([C@@H](Cc2ccccc2Cl)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
44444191 179212 0 None 8 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccccc2Cl)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL447786 179212 0 None 8 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccccc2Cl)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
24936626 24181 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257555 24181 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
19073136 11432 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)c(OC)c1 10.1016/s0960-894x(01)00628-x
CHEMBL103147 11432 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 486 11 4 7 3.4 COc1ccc(C(Cc2ccccc2)NCC(O)c2ccc(O)c(NS(C)(=O)=O)c2)c(OC)c1 10.1016/s0960-894x(01)00628-x
44333802 11850 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 532 12 4 6 5.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(OCc3ccccc3)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL105475 11850 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 532 12 4 6 5.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(OCc3ccccc3)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
18662692 105033 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 469 10 5 6 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C(N)=O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL274494 105033 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 469 10 5 6 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C(N)=O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
19073229 11866 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 427 9 4 6 2.8 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccncc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL105559 11866 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 427 9 4 6 2.8 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccncc2)ccc1O 10.1016/s0960-894x(01)00629-1
18662723 18797 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 491 10 5 7 2.6 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)NC2CCCCC2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL118336 18797 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 491 10 5 7 2.6 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)NC2CCCCC2)cc1 10.1016/j.bmcl.2004.04.074
71623052 151293 16 None -56 2 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000713a ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000713a ADRB3
ChEMBL 558 5 1 6 7.6 Cc1cc(C)c(-n2ccn3nc(-c4cccnc4)cc23)cc1NC(=O)c1cc(C#N)cc(S(F)(F)(F)(F)F)c1 10.6019/CHEMBL5212743
CHEMBL3907057 151293 16 None -56 2 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000713a ADRB3Selectivity interaction (GPCR panel (PDSP screen)) EUB0000713a ADRB3
ChEMBL 558 5 1 6 7.6 Cc1cc(C)c(-n2ccn3nc(-c4cccnc4)cc23)cc1NC(=O)c1cc(C#N)cc(S(F)(F)(F)(F)F)c1 10.6019/CHEMBL5212743
44344619 17829 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 567 10 5 7 4.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL117737 17829 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 567 10 5 7 4.3 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2004.04.074
24937014 24180 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257554 24180 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
46889812 13228 0 None -724 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 415 7 2 4 4.4 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2cccnc2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1082501 13228 0 None -724 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 415 7 2 4 4.4 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2cccnc2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL5274312 200588 0 None -6 5 Human 5.1 pKi = 5.1 Binding
Binding affinity to adrenergic beta 3 (unknown origin)Binding affinity to adrenergic beta 3 (unknown origin)
ChEMBL 383 4 0 3 5.0 CC[Si](C#Cc1cccc2c1OC(C(F)(F)F)C([N+](=O)[O-])=C2)(CC)CC 10.1016/j.bmcl.2022.128981
18435422 161505 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 424 11 4 7 1.5 COc1ccc(CCNCC(O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL399866 161505 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 424 11 4 7 1.5 COc1ccc(CCNCC(O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
18662693 114571 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 483 11 5 6 2.4 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(CC(N)=O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL319186 114571 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 483 11 5 6 2.4 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(CC(N)=O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
24936491 24292 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257916 24292 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
24936492 24321 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258026 24321 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
9821129 211219 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 378 12 3 6 2.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL72169 211219 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 378 12 3 6 2.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
18662711 17808 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL117577 17808 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2004.04.074
18662711 17808 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL117577 17808 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 485 10 5 7 2.8 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2007.05.030
52943730 24105 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 492 9 2 7 5.1 OC(COc1ccccc1)CN1CCC(CNc2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257326 24105 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 492 9 2 7 5.1 OC(COc1ccccc1)CN1CCC(CNc2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
18662704 115966 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 470 9 4 7 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc3c(c2)OCO3)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL321518 115966 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 470 9 4 7 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc3c(c2)OCO3)ccc1O 10.1016/s0960-894x(01)00629-1
10140996 161697 0 None 134 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 486 11 5 7 3.0 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1O 10.1016/j.bmcl.2007.05.030
CHEMBL400947 161697 0 None 134 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 486 11 5 7 3.0 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1O 10.1016/j.bmcl.2007.05.030
24936881 24289 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257913 24289 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
18662719 117105 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 533 10 5 7 3.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL323938 117105 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 533 10 5 7 3.6 COc1ccc([C@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.04.074
18662698 165472 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 497 10 4 6 3.1 CN(C)C(=O)c1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
CHEMBL409312 165472 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 497 10 4 6 3.1 CN(C)C(=O)c1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
52949862 24140 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 464 7 1 7 4.1 OC(COc1ccccc1)CN1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257439 24140 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 464 7 1 7 4.1 OC(COc1ccccc1)CN1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1 10.1016/j.bmcl.2010.08.039
9908924 148433 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL38538 148433 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44333726 11386 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 472 10 4 7 3.2 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL102836 11386 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 472 10 4 7 3.2 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/s0960-894x(01)00628-x
44333588 11429 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 558 12 4 7 4.6 CC(NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(c1ccc(OC(F)F)cc1)c1ccc(OC(F)F)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL103131 11429 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 558 12 4 7 4.6 CC(NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(c1ccc(OC(F)F)cc1)c1ccc(OC(F)F)cc1 10.1016/s0960-894x(01)00628-x
44333726 11386 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 472 10 4 7 3.2 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL102836 11386 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 472 10 4 7 3.2 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.04.074
44333726 11386 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 472 10 4 7 3.2 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL102836 11386 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 472 10 4 7 3.2 COc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2007.05.030
44344526 18398 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 379 8 5 6 1.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCC(=O)Nc2ccccc2)ccc1O 10.1016/j.bmcl.2004.04.074
CHEMBL118069 18398 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 379 8 5 6 1.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCC(=O)Nc2ccccc2)ccc1O 10.1016/j.bmcl.2004.04.074
44334144 11283 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 444 9 4 5 3.5 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc(F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL102177 11283 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 444 9 4 5 3.5 CS(=O)(=O)Nc1cc(C(O)CNC(Cc2ccccc2)c2ccc(F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
44333853 11766 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 524 11 4 6 4.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(OCC(F)(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL104988 11766 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 524 11 4 6 4.3 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(OCC(F)(F)F)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
44333920 11771 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 484 10 4 7 3.2 COC(=O)c1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
CHEMBL105004 11771 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 484 10 4 7 3.2 COC(=O)c1ccc([C@@H](Cc2ccccc2)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/s0960-894x(01)00629-1
52943969 24567 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 517 9 3 8 4.3 CC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258825 24567 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 517 9 3 8 4.3 CC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
46889642 13727 0 None -6 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084527 13727 0 None -6 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2010.04.009
52943919 24493 0 None -14 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 500 10 2 7 5.1 C=CCc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258597 24493 0 None -14 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 500 10 2 7 5.1 C=CCc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
155770281 184526 0 None 1 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to beta3 (unknown origin)Binding affinity to beta3 (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 184526 0 None 1 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to beta3 (unknown origin)Binding affinity to beta3 (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
18662695 115407 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 470 10 5 6 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C(=O)O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL320667 115407 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 470 10 5 6 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(C(=O)O)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
19073112 114324 0 None - 1 Human 4.1 pKi = 4.1 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 450 13 5 6 2.6 CS(=O)(=O)Nc1cc(C(O)CNC(CCCCC(=O)O)Cc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
CHEMBL318830 114324 0 None - 1 Human 4.1 pKi = 4.1 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 450 13 5 6 2.6 CS(=O)(=O)Nc1cc(C(O)CNC(CCCCC(=O)O)Cc2ccccc2)ccc1O 10.1016/s0960-894x(01)00628-x
24886595 24418 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccc(F)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258370 24418 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccc(F)cc1 10.1016/j.bmcl.2010.08.039
44444165 161775 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 520 13 4 6 4.2 CS(=O)(=O)Nc1cc(CC[C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL401334 161775 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 520 13 4 6 4.2 CS(=O)(=O)Nc1cc(CC[C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O 10.1016/j.bmcl.2007.05.030
18662718 18609 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 519 10 5 7 3.4 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL118216 18609 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 519 10 5 7 3.4 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)Nc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.04.074
44333536 114127 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 506 11 4 6 4.1 C[C@](Cc1ccccc1)(NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)c1ccc(OC(F)F)cc1 10.1016/s0960-894x(01)00629-1
CHEMBL317648 114127 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 506 11 4 6 4.1 C[C@](Cc1ccccc1)(NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)c1ccc(OC(F)F)cc1 10.1016/s0960-894x(01)00629-1
9828292 207625 10 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 526 11 4 6 4.6 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2cccc(Cl)c2)c2ccc(OC(F)F)cc2)ccc1O 10.1021/jm980521l
CHEMBL60116 207625 10 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Beta-3 adrenergic receptorBinding affinity towards human Beta-3 adrenergic receptor
ChEMBL 526 11 4 6 4.6 CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2cccc(Cl)c2)c2ccc(OC(F)F)cc2)ccc1O 10.1021/jm980521l
24936885 24255 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257797 24255 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
10207208 160946 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL398557 160946 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
44444185 161537 0 None 43 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 514 13 4 7 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL400067 161537 0 None 43 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
ChEMBL 514 13 4 7 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
52947060 24355 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 474 8 2 7 4.7 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258144 24355 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 474 8 2 7 4.7 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
46889853 13305 0 None -45708 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 458 8 2 5 4.7 COc1ccc(C(=O)C2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1082828 13305 0 None -45708 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 458 8 2 5 4.7 COc1ccc(C(=O)C2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
24937387 24138 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1ccc(O)cc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257437 24138 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1ccc(O)cc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
3339 210420 117 None -10 5 Human 4.0 pKi = 4.0 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1 nan
CHEMBL672 210420 117 None -10 5 Human 4.0 pKi = 4.0 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1 nan
44444151 161715 0 None - 1 Human 7.0 pKi = 7.0 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 635 15 5 10 3.8 CCOP(=O)(OCC)c1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1007/s00044-009-9257-x
CHEMBL401068 161715 0 None - 1 Human 7.0 pKi = 7.0 Binding
Agonist activity at Homo sapiens (human) beta3 adrenoreceptorAgonist activity at Homo sapiens (human) beta3 adrenoreceptor
ChEMBL 635 15 5 10 3.8 CCOP(=O)(OCC)c1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1 10.1007/s00044-009-9257-x
9895810 117358 5 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 649 16 5 10 4.7 CCOP(=O)(Cc1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1)OCC 10.1016/j.bmcl.2004.04.074
CHEMBL325425 117358 5 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 649 16 5 10 4.7 CCOP(=O)(Cc1ccc(NC(=O)[C@@](C)(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(OC)cc2)cc1)OCC 10.1016/j.bmcl.2004.04.074
52943770 24139 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 492 8 4 9 3.8 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257438 24139 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 492 8 4 9 3.8 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
44344701 20960 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 547 9 5 6 3.7 C[C@@](NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(C(=O)Nc1ccccc1)c1ccc(Br)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL119875 20960 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 547 9 5 6 3.7 C[C@@](NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1)(C(=O)Nc1ccccc1)c1ccc(Br)cc1 10.1016/j.bmcl.2004.04.074
567 7512 16 None -1 5 Human 6.0 pKi = 6.0 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
9841972 7512 16 None -1 5 Human 6.0 pKi = 6.0 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
CHEMBL284782 7512 16 None -1 5 Human 6.0 pKi = 6.0 Binding
Ability to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-3 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
567 7512 16 None -1 5 Human 6.0 pKi = 6.0 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
9841972 7512 16 None -1 5 Human 6.0 pKi = 6.0 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
CHEMBL284782 7512 16 None -1 5 Human 6.0 pKi = 6.0 Binding
Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta3 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
18662714 121526 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 465 9 5 7 2.1 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2004.04.074
CHEMBL333879 121526 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cellsBinding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
ChEMBL 465 9 5 7 2.1 COc1ccc([C@H](NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2004.04.074
46889809 13419 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 519 6 2 5 5.0 O=C1c2cccc3cccc(c23)C(=O)N1C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083363 13419 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta3 receptor expressed in CHOK1 cells
ChEMBL 519 6 2 5 5.0 O=C1c2cccc3cccc(c23)C(=O)N1C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
44333790 116540 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 500 12 4 7 3.5 COCc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(COC)cc2)cc1 10.1016/s0960-894x(01)00628-x
CHEMBL323091 116540 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 500 12 4 7 3.5 COCc1ccc(C(NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c2ccc(COC)cc2)cc1 10.1016/s0960-894x(01)00628-x
24936627 24458 0 None -4 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 444 8 4 9 2.2 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258485 24458 0 None -4 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
ChEMBL 444 8 4 9 2.2 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
2303 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 9961 68 None -213 26 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
44333830 11367 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 518 11 4 6 5.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(Oc3ccccc3)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
CHEMBL102701 11367 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindololBinding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 518 11 4 6 5.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC(Cc2ccccc2)c2ccc(Oc3ccccc3)cc2)ccc1O 10.1016/s0960-894x(01)00629-1
155774 10868 40 None -9 3 Human 8.3 pKd = 8.3 Binding
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
2848 10868 40 None -9 3 Human 8.3 pKd = 8.3 Binding
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
538 10868 40 None -9 3 Human 8.3 pKd = 8.3 Binding
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
CHEMBL75753 10868 40 None -9 3 Human 8.3 pKd = 8.3 Binding
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
DB13781 10868 40 None -9 3 Human 8.3 pKd = 8.3 Binding
Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
2176 9901 68 None -151 27 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 None -151 27 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 None -151 27 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 None -151 27 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 None -151 27 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
137 7158 52 None -74 12 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 7158 52 None -74 12 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 7158 52 None -74 12 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 7158 52 None -74 12 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 7158 52 None -74 12 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 7158 52 None -74 12 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2687 7676 16 None -158 5 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 20590599
532 7676 16 None -158 5 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 20590599
5387 7676 16 None -158 5 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 20590599
CHEMBL420746 7676 16 None -158 5 Human 7.0 pKd = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 20590599
3075702 224111 0 125I-CYP -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1028 7079 71 125I-CYP -4168 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 125I-CYP -4168 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 125I-CYP -4168 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 125I-CYP -4168 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 125I-CYP -4168 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 125I-CYP -4168 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
179 7188 115 125I-Iodopindolol -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 125I-Iodopindolol -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 125I-Iodopindolol -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 125I-Iodopindolol -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 125I-Iodopindolol -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2249 7300 111 125I-CYP -295 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 7300 111 125I-CYP -295 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 7300 111 125I-CYP -295 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 7300 111 125I-CYP -295 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 7300 111 125I-CYP -295 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
1155 8410 53 125I-CYP -26 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3343 8410 53 125I-CYP -26 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
557 8410 53 125I-CYP -26 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
CHEMBL32800 8410 53 125I-CYP -26 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
DB01288 8410 53 125I-CYP -26 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
1786 9298 85 125I-CYP -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 9298 85 125I-CYP -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 9298 85 125I-CYP -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 9298 85 125I-CYP -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 9298 85 125I-CYP -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
243 9976 91 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
105 10234 91 125I-CYP -5 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 10234 91 125I-CYP -5 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 10234 91 125I-CYP -5 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 10234 91 125I-CYP -5 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 10234 91 125I-CYP -5 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2598 10550 58 125I-CYP -67 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
5403 10550 58 125I-CYP -67 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
560 10550 58 125I-CYP -67 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
CHEMBL1760 10550 58 125I-CYP -67 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
DB00871 10550 58 125I-CYP -67 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
1499 8872 47 125I-CYP -588 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 125I-CYP -588 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 125I-CYP -588 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 125I-CYP -588 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 125I-CYP -588 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
2303 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 125I-CYP -213 26 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
2685 7677 21 125I-CYP -2630 7 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O None
541 7677 21 125I-CYP -2630 7 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O None
CHEMBL280822 7677 21 125I-CYP -2630 7 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O None
2585 7590 103 125I-CYP -16 22 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 7590 103 125I-CYP -16 22 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 7590 103 125I-CYP -16 22 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 7590 103 125I-CYP -16 22 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 7590 103 125I-CYP -16 22 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
137 7158 52 125I-CYP -74 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 7158 52 125I-CYP -74 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 7158 52 125I-CYP -74 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 7158 52 125I-CYP -74 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 7158 52 125I-CYP -74 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 7158 52 125I-CYP -74 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
71149 223177 0 125I-CYP -3 3 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 262 3 2 4 1.9 CC(C)(C)NCC(C1=CC(=NO1)Br)O None
3339 210420 117 None -10 5 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1 None
CHEMBL672 210420 117 None -10 5 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1 None
176 7186 66 None -10 31 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 7186 66 None -10 31 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 7186 66 None -10 31 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 7186 66 None -10 31 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 7186 66 None -10 31 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
64143 205643 62 None -1 8 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C None
CHEMBL584 205643 62 None -1 8 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C None
105 10234 91 125I-ICYP -5 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 10234 91 125I-ICYP -5 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 10234 91 125I-ICYP -5 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 10234 91 125I-ICYP -5 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 10234 91 125I-ICYP -5 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1212 8443 50 None -630 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -630 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -630 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -630 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -630 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
28417 46813 49 None -2 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL1479 46813 49 None -2 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
2662 18156 131 None 1 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 18156 131 None 1 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
None 223176 0 125I-CYP 21 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 363 9 3 4 3.1 CC(CC1=CC=C(C=C1)OCC(=O)O)NCC(C2=CC(=CC=C2)Cl)O None
484 9633 51 125I-CYP -42 35 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 125I-CYP -42 35 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 125I-CYP -42 35 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2176 9901 68 125I-CYP -151 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-CYP -151 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-CYP -151 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-CYP -151 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-CYP -151 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2405 7452 76 None -32 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
380 7452 76 None -32 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
7129 7452 76 None -32 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
CHEMBL645 7452 76 None -32 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
DB00612 7452 76 None -32 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
2247 7293 81 None -102 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 None -102 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 None -102 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 None -102 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 None -102 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1016 10519 78 None -33 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 10519 78 None -33 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 10519 78 None -33 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 10519 78 None -33 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 10519 78 None -33 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 10519 78 None -33 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
11504295 9697 47 None 1 3 Human 8.3 pKi = 8.3 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
4814 9697 47 None 1 3 Human 8.3 pKi = 8.3 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
7543 9697 47 None 1 3 Human 8.3 pKi = 8.3 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
CHEMBL605846 9697 47 None 1 3 Human 8.3 pKi = 8.3 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
DB09080 9697 47 None 1 3 Human 8.3 pKi = 8.3 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
2812 11551 101 None -35 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None -35 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1499 8872 47 None -44 17 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
1499 8872 47 None -23 17 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 None -44 17 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 None -23 17 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 None -44 17 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 None -23 17 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 None -44 17 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 None -23 17 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 None -44 17 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 None -23 17 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3198 212292 76 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 212292 76 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 212292 76 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1548955 95356 20 None -1 18 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 95356 20 None -1 18 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 95356 20 None -1 18 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
4189 213701 96 None -28 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 213701 96 None -28 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 213701 96 None -28 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
657255 205863 34 None -21 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 205863 34 None -21 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
5353853 24758 47 None -25 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 24758 47 None -25 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 24758 47 None -25 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2540 11173 111 None 1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 None
CHEMBL1014 11173 111 None 1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 None
3083544 33582 51 125I-ICYP -43 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1200811 33582 51 125I-ICYP -43 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1363 33582 51 125I-ICYP -43 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1951071 33582 51 125I-ICYP -43 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL605993 33582 51 125I-ICYP -43 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
1836 9370 59 None -61 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 9370 59 None -61 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 9370 59 None -61 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 9370 59 None -61 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 9370 59 None -61 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
2419 10236 84 125I-ICYP -53 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 10236 84 125I-ICYP -53 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 10236 84 125I-ICYP -53 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 10236 84 125I-ICYP -53 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 10236 84 125I-ICYP -53 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
107715 207724 22 None -281 20 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 207724 22 None -281 20 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 207724 22 None -281 20 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
118422671 9533 65 None -19 4 Human 8.3 pKi = 8.3 Binding
Radioligand bindingRadioligand binding
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
1887 9533 65 None -19 4 Human 8.3 pKi = 8.3 Binding
Radioligand bindingRadioligand binding
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
71301 9533 65 None -19 4 Human 8.3 pKi = 8.3 Binding
Radioligand bindingRadioligand binding
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
7246 9533 65 None -19 4 Human 8.3 pKi = 8.3 Binding
Radioligand bindingRadioligand binding
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
CHEMBL434394 9533 65 None -19 4 Human 8.3 pKi = 8.3 Binding
Radioligand bindingRadioligand binding
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
DB04861 9533 65 None -19 4 Human 8.3 pKi = 8.3 Binding
Radioligand bindingRadioligand binding
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
3191 109635 97 None -20 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 109635 97 None -20 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
134551 7146 27 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 7146 27 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 7146 27 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 7146 27 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
2303 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 None -213 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
33630 185736 99 None -10 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assayDisplacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 185736 99 None -10 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assayDisplacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in HEK293FlpIN cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
3914 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
39468 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
431 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
570 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
CHEMBL1201237 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
CHEMBL293030 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
DB01210 7527 35 None -42 7 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
11823027 199395 37 None 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
4411 199395 37 None 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
CHEMBL521606 199395 37 None 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
3914 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
39468 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
431 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
570 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
CHEMBL1201237 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
CHEMBL293030 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
DB01210 7527 35 None -36 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
44112 128068 48 None -7 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
CHEMBL357995 128068 48 None -7 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
33624 10593 34 None -87 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
4061 10593 34 None -87 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
565 10593 34 None -87 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
CHEMBL499 10593 34 None -87 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
DB00373 10593 34 None -87 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
2291 9958 58 None -8 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 9958 58 None -8 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 9958 58 None -8 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 9958 58 None -8 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 9958 58 None -8 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
3914 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
39468 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
431 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
570 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
CHEMBL1201237 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
CHEMBL293030 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
DB01210 7527 35 None -45 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O None
2303 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 None -93 26 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
3682 196216 12 125I-CYP -1202 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 196216 12 125I-CYP -1202 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 196216 12 125I-CYP -1202 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
2605 10555 30 None -5 10 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
2605 10555 30 None -5 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 10555 30 None -5 10 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 10555 30 None -5 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 10555 30 None -5 10 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 10555 30 None -5 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 10555 30 None -5 10 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 10555 30 None -5 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 10555 30 None -5 10 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 10555 30 None -5 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
2475 7528 0 None -9 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
433 7528 0 None -9 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
550 7528 0 None -9 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
CHEMBL305380 7528 0 None -9 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
DB08808 7528 0 None -9 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
487 7580 71 None -112 7 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
487 7580 71 None -112 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
569 7580 71 None -112 7 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
569 7580 71 None -112 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
71739 7580 71 None -112 7 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
71739 7580 71 None -112 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
CHEMBL324665 7580 71 None -112 7 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
CHEMBL324665 7580 71 None -112 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
2419 10236 84 125I-CYP -53 6 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 10236 84 125I-CYP -53 6 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 10236 84 125I-CYP -53 6 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 10236 84 125I-CYP -53 6 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 10236 84 125I-CYP -53 6 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
2687 7676 16 125I-CYP -158 5 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
532 7676 16 125I-CYP -158 5 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
5387 7676 16 125I-CYP -158 5 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
CHEMBL420746 7676 16 125I-CYP -158 5 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
2605 10555 30 None 1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 10555 30 None 1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 10555 30 None 1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 10555 30 None 1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 10555 30 None 1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
487 7580 71 None -52 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
569 7580 71 None -52 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
71739 7580 71 None -52 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
CHEMBL324665 7580 71 None -52 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
3083544 33582 51 125I-CYP -43 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1200811 33582 51 125I-CYP -43 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1363 33582 51 125I-CYP -43 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL1951071 33582 51 125I-CYP -43 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
CHEMBL605993 33582 51 125I-CYP -43 5 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 None
2585 7590 103 None -16 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 7590 103 None -16 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 7590 103 None -16 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 7590 103 None -16 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 7590 103 None -16 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
2405 7452 76 125I-CYP -32 4 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
380 7452 76 125I-CYP -32 4 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
7129 7452 76 125I-CYP -32 4 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
CHEMBL645 7452 76 125I-CYP -32 4 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
DB00612 7452 76 125I-CYP -32 4 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
118422671 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 20590599
118422671 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
1887 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 20590599
1887 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
71301 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 20590599
71301 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
7246 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 20590599
7246 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
CHEMBL434394 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 20590599
CHEMBL434394 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
DB04861 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 20590599
DB04861 9533 65 None -19 4 Human 6.3 pKi = 6.3 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
1960 9632 67 None -32359 26 Mouse 3.8 pKi = 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
439260 9632 67 None -32359 26 Mouse 3.8 pKi = 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
505 9632 67 None -32359 26 Mouse 3.8 pKi = 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
CHEMBL1437 9632 67 None -32359 26 Mouse 3.8 pKi = 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
DB00368 9632 67 None -32359 26 Mouse 3.8 pKi = 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
1960 9632 67 None -12882 26 Rat 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
439260 9632 67 None -12882 26 Rat 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
505 9632 67 None -12882 26 Rat 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
CHEMBL1437 9632 67 None -12882 26 Rat 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
DB00368 9632 67 None -12882 26 Rat 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
1028 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
1028 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
139148732 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
139148732 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
479 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
479 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
5816 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
5816 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
CHEMBL679 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
CHEMBL679 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
DB00668 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
DB00668 7079 71 None -4168 30 Human 4.3 pKi = 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 20590599
146015362 7734 10 None -8 3 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 11249148
3462 7734 10 None -8 3 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 11249148
5486546 7734 10 None -8 3 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 11249148
CHEMBL1204876 7734 10 None -8 3 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 11249148
12578 7723 61 None -19 2 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 20590599
2755 7723 61 None -19 2 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 20590599
CHEMBL1374751 7723 61 None -19 2 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 20590599
2685 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10079020
2685 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10411574
2685 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 15655528
2685 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 8719421
541 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10079020
541 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10411574
541 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 15655528
541 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 8719421
CHEMBL280822 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10079020
CHEMBL280822 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10411574
CHEMBL280822 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 15655528
CHEMBL280822 7677 21 None -2630 7 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 8719421
1155 8410 53 None -26 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
3343 8410 53 None -26 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
557 8410 53 None -26 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
CHEMBL32800 8410 53 None -26 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
DB01288 8410 53 None -26 5 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 20590599
1960 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
1960 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
1960 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9131260
439260 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
439260 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
439260 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9131260
505 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
505 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
505 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9131260
CHEMBL1437 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
CHEMBL1437 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
CHEMBL1437 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9131260
DB00368 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
DB00368 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14744619
DB00368 9632 67 None -26 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9131260
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14730417
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9117106
1499 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9131260
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14730417
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9117106
3779 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9131260
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14730417
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9117106
536 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9131260
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14730417
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9117106
CHEMBL434 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9131260
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14730417
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 20590599
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9117106
DB01064 8872 47 None -588 17 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 9131260
146015362 7734 10 None 8 3 Mouse 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
3462 7734 10 None 8 3 Mouse 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
5486546 7734 10 None 8 3 Mouse 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
CHEMBL1204876 7734 10 None 8 3 Mouse 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 17717109
5311179 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
5311179 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 14730417
5311179 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
5311179 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 8719421
543 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
543 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 14730417
543 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
543 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 8719421
5484725 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
5484725 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 14730417
5484725 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
5484725 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 8719421
CHEMBL1233766 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
CHEMBL1233766 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 14730417
CHEMBL1233766 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
CHEMBL1233766 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 8719421
CHEMBL198059 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
CHEMBL198059 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 14730417
CHEMBL198059 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
CHEMBL198059 8755 21 None -295 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 8719421
3914 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
39468 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
431 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
570 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
CHEMBL1201237 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
CHEMBL293030 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
DB01210 7527 35 None -42 7 Mouse 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
39147 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
39147 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
554 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
554 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
CHEMBL649 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
CHEMBL649 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
DB01203 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
DB01203 9489 0 None -35 3 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
3914 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
39468 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
431 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
570 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
CHEMBL1201237 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
CHEMBL293030 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
DB01210 7527 35 None -36 7 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
2303 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
4946 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
564 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
63 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
91536 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
CHEMBL27 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
CHEMBL452861 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
DB00571 9961 68 None -870 26 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
567 7512 16 None 1 5 Mouse 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
9841972 7512 16 None 1 5 Mouse 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
CHEMBL284782 7512 16 None 1 5 Mouse 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
2303 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
4946 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
564 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
63 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
91536 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
CHEMBL27 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
CHEMBL452861 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
DB00571 9961 68 None -93 26 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
2687 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
2687 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 7903415
2687 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
2687 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 9117106
532 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
532 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 7903415
532 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
532 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 9117106
5387 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
5387 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 7903415
5387 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
5387 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 9117106
CHEMBL420746 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
CHEMBL420746 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 7903415
CHEMBL420746 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
CHEMBL420746 7676 16 None -158 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 9117106
567 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 14730417
567 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 7903415
567 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 7912272
567 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
9841972 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 14730417
9841972 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 7903415
9841972 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 7912272
9841972 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
CHEMBL284782 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 14730417
CHEMBL284782 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 7903415
CHEMBL284782 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 7912272
CHEMBL284782 7512 16 None -1 5 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
2303 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
2303 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
2303 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
4946 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
4946 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
4946 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
564 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
564 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
564 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
63 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
63 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
63 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
91536 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
91536 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
91536 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
CHEMBL27 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
CHEMBL27 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
CHEMBL27 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
CHEMBL452861 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
CHEMBL452861 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
CHEMBL452861 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
DB00571 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10079020
DB00571 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 14744619
DB00571 9961 68 None -213 26 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 15655528
3914 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
39468 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
431 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
570 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
CHEMBL1201237 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
CHEMBL293030 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
DB01210 7527 35 None -45 7 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 CC(C)(C)NCC(COC1=CC=CC2=C1CCCC2=O)O 14744619
2475 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
2475 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
2475 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 7903415
2475 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 8719421
433 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
433 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
433 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 7903415
433 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 8719421
550 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
550 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
550 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 7903415
550 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 8719421
CHEMBL305380 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
CHEMBL305380 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
CHEMBL305380 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 7903415
CHEMBL305380 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 8719421
DB08808 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
DB08808 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
DB08808 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 7903415
DB08808 7528 0 None -9 3 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 8719421
2176 9901 68 None -151 27 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
4828 9901 68 None -151 27 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
91 9901 68 None -151 27 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
CHEMBL500 9901 68 None -151 27 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
DB00960 9901 68 None -151 27 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 20590599
5311452 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 10411574
5311452 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 14730417
5311452 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 20590599
5311452 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 8730727
547 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 10411574
547 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 14730417
547 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 20590599
547 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 8730727
CHEMBL1326499 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 10411574
CHEMBL1326499 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 14730417
CHEMBL1326499 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 20590599
CHEMBL1326499 10443 11 None -17 3 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 8730727
10028830 9026 40 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10411574
10028830 9026 40 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
3932 9026 40 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10411574
3932 9026 40 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
CHEMBL4238084 9026 40 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10411574
CHEMBL4238084 9026 40 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
487 7580 71 None -52 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
569 7580 71 None -52 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
71739 7580 71 None -52 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
CHEMBL324665 7580 71 None -52 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 20590599
10323892 9025 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 505 12 4 7 1.7 O[C@H](COc1cccc(c1)S(=O)(=O)N)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10411574
10323892 9025 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 505 12 4 7 1.7 O[C@H](COc1cccc(c1)S(=O)(=O)N)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
3463 9025 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 505 12 4 7 1.7 O[C@H](COc1cccc(c1)S(=O)(=O)N)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10411574
3463 9025 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 505 12 4 7 1.7 O[C@H](COc1cccc(c1)S(=O)(=O)N)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
CHEMBL1628562 9025 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 505 12 4 7 1.7 O[C@H](COc1cccc(c1)S(=O)(=O)N)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10411574
CHEMBL1628562 9025 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 505 12 4 7 1.7 O[C@H](COc1cccc(c1)S(=O)(=O)N)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 20590599
2585 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
2585 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
522 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
522 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
551 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
551 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
CHEMBL723 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
CHEMBL723 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
DB01136 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
DB01136 7590 103 None -16 22 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
1960 9632 67 None -26 26 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 9632 67 None -26 26 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 9632 67 None -26 26 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 9632 67 None -26 26 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 9632 67 None -26 26 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
4508 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 14730417
4508 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 7903415
4508 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
4866774 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 14730417
4866774 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 7903415
4866774 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
509 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 14730417
509 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 7903415
509 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
838 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 14730417
838 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 7903415
838 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
CHEMBL1740 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 14730417
CHEMBL1740 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 7903415
CHEMBL1740 9913 98 None -10000 13 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
1499 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
1499 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
3779 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
3779 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
536 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
536 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
CHEMBL434 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
CHEMBL434 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
DB01064 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 14744619
DB01064 8872 47 None -44 17 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
3035442 7184 0 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 8 2 5 3.5 CCOC(=O)COc1ccc2c(c1)C[C@H](CC2)NC[C@@H](c1cccc(c1)Cl)O 7903415
568 7184 0 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 8 2 5 3.5 CCOC(=O)COc1ccc2c(c1)C[C@H](CC2)NC[C@@H](c1cccc(c1)Cl)O 7903415
CHEMBL1193948 7184 0 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 8 2 5 3.5 CCOC(=O)COc1ccc2c(c1)C[C@H](CC2)NC[C@@H](c1cccc(c1)Cl)O 7903415
DB05395 7184 0 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 8 2 5 3.5 CCOC(=O)COc1ccc2c(c1)C[C@H](CC2)NC[C@@H](c1cccc(c1)Cl)O 7903415
1499 8872 47 None -23 17 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
3779 8872 47 None -23 17 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
536 8872 47 None -23 17 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
CHEMBL434 8872 47 None -23 17 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
DB01064 8872 47 None -23 17 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8719421
4508 9913 98 None -1000 13 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
4508 9913 98 None -1000 13 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
4866774 9913 98 None -1000 13 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
4866774 9913 98 None -1000 13 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
509 9913 98 None -1000 13 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
509 9913 98 None -1000 13 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
838 9913 98 None -1000 13 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
838 9913 98 None -1000 13 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
CHEMBL1740 9913 98 None -1000 13 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
CHEMBL1740 9913 98 None -1000 13 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 8719421
567 7512 16 None -1 5 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
9841972 7512 16 None -1 5 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
CHEMBL284782 7512 16 None -1 5 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 8719421
2687 7676 16 None -218 5 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
2687 7676 16 None -218 5 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
532 7676 16 None -218 5 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
532 7676 16 None -218 5 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
5387 7676 16 None -218 5 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
5387 7676 16 None -218 5 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
CHEMBL420746 7676 16 None -218 5 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
CHEMBL420746 7676 16 None -218 5 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 8719421
2605 10555 30 None -5 10 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
2605 10555 30 None -5 10 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
36920 10555 30 None -5 10 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
36920 10555 30 None -5 10 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
571 10555 30 None -5 10 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
571 10555 30 None -5 10 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
CHEMBL434200 10555 30 None -5 10 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
CHEMBL434200 10555 30 None -5 10 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
DB13775 10555 30 None -5 10 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
DB13775 10555 30 None -5 10 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
487 7580 71 None -112 7 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
487 7580 71 None -112 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
569 7580 71 None -112 7 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
569 7580 71 None -112 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
71739 7580 71 None -112 7 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
71739 7580 71 None -112 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
CHEMBL324665 7580 71 None -112 7 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
CHEMBL324665 7580 71 None -112 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 8719421
2605 10555 30 None 1 10 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
36920 10555 30 None 1 10 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
571 10555 30 None 1 10 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
CHEMBL434200 10555 30 None 1 10 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619
DB13775 10555 30 None 1 10 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 14744619