Ligand source activities (1 row/activity)





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

59304608 82034 0 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 82034 0 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
46890269 14146 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086353 14146 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
15605648 82032 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 4 1.1 O=c1[nH]c(=O)c2c(CCCC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036952 82032 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 4 1.1 O=c1[nH]c(=O)c2c(CCCC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
15604638 82037 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 5 2 4 1.3 O=c1[nH]c(=O)c2c(CCCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036957 82037 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 5 2 4 1.3 O=c1[nH]c(=O)c2c(CCCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
145957566 169066 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 169066 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145957566 169066 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 169066 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
156010038 183809 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4632359 183809 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
776464 100484 97 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL247098 100484 97 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.07.101
117629482 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
1588 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
1594 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
2835 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
938 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
CHEMBL573 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
DB00627 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
17751630 13517 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083743 13517 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
117629482 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1588 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1594 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
2835 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
938 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
CHEMBL573 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
DB00627 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
156016715 184454 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
CHEMBL4641756 184454 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
117629482 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1588 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1594 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
2835 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
938 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
CHEMBL573 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
DB00627 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
117629482 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
11594881 95413 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235740 95413 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
117629482 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1588 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1594 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
2835 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
938 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
CHEMBL573 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
DB00627 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
11523095 190966 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 347 7 2 2 4.9 O=C(CCCCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483153 190966 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 347 7 2 2 4.9 O=C(CCCCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
117629482 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1588 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1594 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
2835 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
938 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
CHEMBL573 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
DB00627 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
11594881 95413 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL235740 95413 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
776464 100484 97 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL247098 100484 97 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.06.028
117629482 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1588 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1594 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
2835 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
938 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
CHEMBL573 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
DB00627 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
117629482 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1588 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1594 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
2835 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
938 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
CHEMBL573 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
DB00627 9599 140 None -4 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
54585613 68173 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770174 68173 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
57402396 76692 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 236 3 1 5 0.8 CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939012 76692 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 236 3 1 5 0.8 CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
57397200 76695 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 312 5 1 5 2.1 CCc1cc(=O)oc2nc(OCCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939015 76695 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 312 5 1 5 2.1 CCc1cc(=O)oc2nc(OCCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57400597 76714 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 303 4 1 7 1.3 CCc1cc(=O)oc2nc(OCc3cc(C)on3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939034 76714 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 303 4 1 7 1.3 CCc1cc(=O)oc2nc(OCc3cc(C)on3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
145954324 169291 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4167588 169291 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
90645405 119310 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3299113 119310 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
145954324 169291 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4167588 169291 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
11672831 82815 4 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 1 2 2 1.4 CC1(C)C2Cc3c(C(=O)O)n[nH]c3C21 10.1021/jm2010964
CHEMBL2057235 82815 4 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 1 2 2 1.4 CC1(C)C2Cc3c(C(=O)O)n[nH]c3C21 10.1021/jm2010964
776416 25710 108 None -5 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL128604 25710 108 None -5 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
11550911 101963 1 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL255877 101963 1 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
57397201 76703 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccc(OC)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939023 76703 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccc(OC)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
53325342 64812 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 336 6 1 4 3.3 O=c1cc(CCCC2(C3CC3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672642 64812 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 336 6 1 4 3.3 O=c1cc(CCCC2(C3CC3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
24954941 64815 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 4 1 4 2.5 O=c1cc(CCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672732 64815 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 4 1 4 2.5 O=c1cc(CCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
11159621 9326 46 None 1 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 9326 46 None 1 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 9326 46 None 1 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 9326 46 None 1 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
776421 96703 108 None 30 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL238002 96703 108 None 30 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
13153555 100638 27 None 42 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL247921 100638 27 None 42 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
46890327 13372 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083138 13372 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
59304946 82022 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 268 4 2 5 0.5 CSCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036828 82022 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 268 4 2 5 0.5 CSCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11483496 6914 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
1589 6914 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
CHEMBL375493 6914 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
11483496 6914 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1589 6914 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL375493 6914 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
135416383 191688 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485326 191688 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
59304655 82021 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 252 4 2 5 -0.3 COCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036827 82021 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 252 4 2 5 -0.3 COCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
137652577 165539 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093990 165539 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11184165 90229 0 None 5 2 Human 6.0 pEC50 = 6.0 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 246 3 1 3 2.0 CCc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL219950 90229 0 None 5 2 Human 6.0 pEC50 = 6.0 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 246 3 1 3 2.0 CCc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
12003788 201720 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 201720 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 201720 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
12003787 202621 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL558463 202621 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
16048917 160793 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc12 10.1016/j.bmcl.2007.10.055
CHEMBL398414 160793 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc12 10.1016/j.bmcl.2007.10.055
135401974 161502 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL399859 161502 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
46889338 13496 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1083683 13496 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
53317449 64835 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 222 2 2 5 -0.1 CCc1cc(=O)oc2nc(CO)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672767 64835 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 222 2 2 5 -0.1 CCc1cc(=O)oc2nc(CO)[nH]c(=O)c12 10.1021/ml100251u
57413448 83126 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 234 5 2 2 2.6 CCCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059226 83126 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 234 5 2 2 2.6 CCCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
57395376 76701 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939021 76701 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57412210 82890 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@H]12 10.1021/jm2010964
CHEMBL2057616 82890 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@H]12 10.1021/jm2010964
15605571 82010 2 None -1 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 82010 2 None -1 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
49763030 82892 31 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 O=C(O)c1n[nH]c2c1C[C@H]1C[C@@H]21 10.1021/jm2010964
CHEMBL2057618 82892 31 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 O=C(O)c1n[nH]c2c1C[C@H]1C[C@@H]21 10.1021/jm2010964
117629482 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
1588 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
1594 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
2835 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
938 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
CHEMBL573 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
DB00627 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
135800177 152729 7 None 24 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 152729 7 None 24 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11617852 191314 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL484783 191314 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
25101223 7935 7 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
5795 7935 7 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
CHEMBL490599 7935 7 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
117629482 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
1588 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
1594 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
2835 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
938 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
CHEMBL573 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
DB00627 9599 140 None -4 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
135800177 152729 7 None 24 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL391813 152729 7 None 24 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11992586 202279 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 217 4 3 3 1.7 O=C(O)c1cc(NCc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL553435 202279 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 217 4 3 3 1.7 O=C(O)c1cc(NCc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
11160694 144934 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2cccc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL376889 144934 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2cccc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
4268702 176431 8 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
CHEMBL443733 176431 8 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
145984458 172274 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 600 7 2 8 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4240407 172274 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 600 7 2 8 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
11322761 148384 1 None 1 2 Human 4.9 pEC50 = 4.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)cc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL385103 148384 1 None 1 2 Human 4.9 pEC50 = 4.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)cc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
44441318 100566 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 228 2 2 2 2.2 O=C(O)c1[nH]nc2c1CCC2c1ccccc1 10.1016/j.bmcl.2007.06.028
CHEMBL247527 100566 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 228 2 2 2 2.2 O=C(O)c1[nH]nc2c1CCC2c1ccccc1 10.1016/j.bmcl.2007.06.028
11845295 156357 42 None -1 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
CHEMBL394688 156357 42 None -1 2 Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
44441310 156062 4 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 4 2 3 0.3 COCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL394464 156062 4 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 4 2 3 0.3 COCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
57393654 76691 2 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 222 2 1 5 0.4 CCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939011 76691 2 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 222 2 1 5 0.4 CCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
882926 92382 13 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm200371q
CHEMBL228244 92382 13 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm200371q
882926 92382 13 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
CHEMBL228244 92382 13 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
90645413 119260 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 4 2 2 4.0 O=C(O)C1=C(NC(=O)[C@@H]2C[C@H]2c2ccc3ccccc3c2)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298703 119260 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 4 2 2 4.0 O=C(O)C1=C(NC(=O)[C@@H]2C[C@H]2c2ccc3ccccc3c2)CCCC1 10.1016/j.bmc.2014.05.011
53326893 64822 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 1 1 4 1.5 CCc1cc(=O)oc2nc(C(F)(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672742 64822 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 1 1 4 1.5 CCc1cc(=O)oc2nc(C(F)(F)F)[nH]c(=O)c12 10.1021/ml100251u
24954204 64830 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 5 1 4 2.5 CCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672751 64830 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 5 1 4 2.5 CCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
57413453 83248 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 190 2 2 2 1.2 C=C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059825 83248 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 190 2 2 2 1.2 C=C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
46889360 13879 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085200 13879 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
15605654 82033 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 248 3 2 4 0.5 O=c1[nH]c(=O)c2c(CCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036953 82033 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 248 3 2 4 0.5 O=c1[nH]c(=O)c2c(CCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
46890299 13987 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085655 13987 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
53322717 64820 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 322 4 1 4 2.9 O=c1cc(CCC2CC3(CC3)C2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672738 64820 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 322 4 1 4 2.9 O=c1cc(CCC2CC3(CC3)C2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
137633734 163100 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4065654 163100 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137641317 163790 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073374 163790 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
1595 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
51576 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
CHEMBL278488 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
1595 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
51576 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
CHEMBL278488 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
1595 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
51576 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
CHEMBL278488 7047 49 None 4 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
24741310 96397 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237543 96397 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44580038 193728 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
CHEMBL490221 193728 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
44579693 193870 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
CHEMBL491396 193870 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
853085 154776 111 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 127 1 1 3 0.7 Cc1cc(C(=O)O)on1 10.1016/j.bmcl.2007.06.028
CHEMBL393428 154776 111 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 127 1 1 3 0.7 Cc1cc(C(=O)O)on1 10.1016/j.bmcl.2007.06.028
12003788 201720 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 201720 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 201720 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
12002717 203521 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
CHEMBL565163 203521 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
15605357 82015 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 224 1 3 5 -0.8 CC(O)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036821 82015 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 224 1 3 5 -0.8 CC(O)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
145984088 172594 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 630 8 2 9 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4248415 172594 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 630 8 2 9 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
16048995 101430 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252505 101430 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
16048992 101457 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252707 101457 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
15605498 76704 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccccc3C(F)(F)F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939024 76704 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccccc3C(F)(F)F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
88707 100532 141 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 201 1 1 2 1.5 O=C(O)c1cncc(Br)c1 10.1016/j.bmcl.2007.06.028
CHEMBL247336 100532 141 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 201 1 1 2 1.5 O=C(O)c1cncc(Br)c1 10.1016/j.bmcl.2007.06.028
24954940 76724 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 336 4 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(Cc3ccccc3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939044 76724 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 336 4 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(Cc3ccccc3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
46890401 14059 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086031 14059 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
57393655 76696 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 266 5 1 6 0.5 CCc1cc(=O)oc2nc(OCCOC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939016 76696 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 266 5 1 6 0.5 CCc1cc(=O)oc2nc(OCCOC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57392461 76646 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 240 1 1 5 -0.1 Cc1cc(=O)oc2nc([S+](C)[O-])[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1938888 76646 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 240 1 1 5 -0.1 Cc1cc(=O)oc2nc([S+](C)[O-])[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11514051 82887 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 1 2 2 1.9 O=C(O)c1n[nH]c2c1CC1C2C12CCCC2 10.1021/jm2010964
CHEMBL2057610 82887 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 1 2 2 1.9 O=C(O)c1n[nH]c2c1CC1C2C12CCCC2 10.1021/jm2010964
135899178 22982 0 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 22982 0 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156016157 184557 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
CHEMBL4643073 184557 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
44579780 193939 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 442 8 1 5 4.8 COCC(Cc1ccccc1)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
CHEMBL492027 193939 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 442 8 1 5 4.8 COCC(Cc1ccccc1)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
117629482 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1588 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1594 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
2835 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
938 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
CHEMBL573 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
DB00627 9599 140 None -4 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
90645401 119258 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 337 4 3 3 3.6 O=C(/C=C/c1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298701 119258 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 337 4 3 3 3.6 O=C(/C=C/c1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
1591 6919 63 None 33 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.06.028
6485181 6919 63 None 33 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL428730 6919 63 None 33 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.06.028
156020831 184849 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647398 184849 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
24954566 64806 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.9 O=c1cc(CCC2CCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672637 64806 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.9 O=c1cc(CCC2CCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57413544 82882 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
CHEMBL2057603 82882 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
46889361 13603 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083988 13603 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
11660694 184847 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647392 184847 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
24955646 64808 0 None -2 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 64808 0 None -2 4 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
156019027 184576 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
CHEMBL4643451 184576 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
156020512 184883 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647933 184883 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12430656 154512 88 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 129 1 1 3 0.8 O=C(O)c1cnsc1 10.1016/j.bmcl.2007.06.028
CHEMBL393226 154512 88 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 129 1 1 3 0.8 O=C(O)c1cnsc1 10.1016/j.bmcl.2007.06.028
136000669 68178 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770179 68178 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
44433527 95309 11 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 150 1 2 4 -0.1 Cc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL235228 95309 11 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 150 1 2 4 -0.1 Cc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
44433531 95312 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 1 2 4 0.0 Cc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL235231 95312 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 1 2 4 0.0 Cc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
46889339 13952 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085534 13952 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
135416394 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
70683908 81815 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 280 4 2 4 1.0 O=c1[nH]c(=O)c2c(CCCC3(F)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2035002 81815 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 280 4 2 4 1.0 O=c1[nH]c(=O)c2c(CCCC3(F)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
59343651 82038 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 5 2 4 1.7 CCC1(CCCc2cc(=O)oc3[nH]c(=O)[nH]c(=O)c23)CC1 10.1021/ml200243g
CHEMBL2036959 82038 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 5 2 4 1.7 CCC1(CCCc2cc(=O)oc3[nH]c(=O)[nH]c(=O)c23)CC1 10.1021/ml200243g
57413367 82888 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057614 82888 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
137635325 162928 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4063682 162928 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11322738 143544 1 None 13 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 252 2 1 3 2.1 CC1(c2cccc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL374111 143544 1 None 13 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 252 2 1 3 2.1 CC1(c2cccc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
136375410 184096 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4636989 184096 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
16048770 101406 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252306 101406 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
59304808 82012 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 1 2 4 0.3 O=c1[nH]c(=O)c2c(CC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036816 82012 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 1 2 4 0.3 O=c1[nH]c(=O)c2c(CC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
135800177 152729 7 None -24 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 152729 7 None -24 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135899325 22965 0 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 22965 0 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
1592 6932 131 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 10.1016/j.bmcl.2007.06.028
256208 6932 131 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL247132 6932 131 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 10.1016/j.bmcl.2007.06.028
44441302 100130 23 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL245491 100130 23 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.06.028
57412217 83123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2059223 83123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
11159621 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
145957566 169066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 169066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145957566 169066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 169066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
21660892 154296 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 136 1 2 4 -0.4 c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393063 154296 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 136 1 2 4 -0.4 c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
136086823 13741 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1084576 13741 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
15605571 82010 2 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 82010 2 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
117629482 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1588 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1594 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
2835 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
938 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
CHEMBL573 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
DB00627 9599 140 None -4 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
135399731 190936 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
CHEMBL482963 190936 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
70681781 82014 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 288 2 2 4 0.9 O=c1[nH]c(=O)c2c(Cc3ccc(F)cc3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036820 82014 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 288 2 2 4 0.9 O=c1[nH]c(=O)c2c(Cc3ccc(F)cc3)cc(=O)oc2[nH]1 10.1021/ml200243g
136127010 22858 11 None -9 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 22858 11 None -9 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048843 161170 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
CHEMBL398762 161170 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
24953857 76726 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 342 5 1 5 2.8 CCC#CCOc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939046 76726 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 342 5 1 5 2.8 CCC#CCOc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
57400598 76720 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 3 1 5 2.4 CCc1cc(=O)oc2nc(OCC#CC3CCCCC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939040 76720 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 3 1 5 2.4 CCc1cc(=O)oc2nc(OCC#CC3CCCCC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57413446 83122 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059222 83122 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
24954572 76722 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 2 6 0.2 CCc1cc(=O)oc2nc(OCC#CCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939042 76722 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 2 6 0.2 CCc1cc(=O)oc2nc(OCC#CCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
44579646 193744 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccccc2F)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490413 193744 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccccc2F)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
13153555 100638 27 None 42 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL247921 100638 27 None 42 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
676464 96651 75 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL237788 96651 75 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
44433529 95311 0 None -5 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 176 2 2 4 0.5 c1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
CHEMBL235230 95311 0 None -5 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 176 2 2 4 0.5 c1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
46889397 13497 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 232 3 2 5 0.1 COC[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083688 13497 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 232 3 2 5 0.1 COC[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
44433530 154302 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 192 4 2 4 0.9 CCCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393065 154302 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 192 4 2 4 0.9 CCCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
135416384 191603 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL485196 191603 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
15605645 82019 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 4 2 4 0.9 CCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036825 82019 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 4 2 4 0.9 CCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
57397199 76694 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939014 76694 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
135899171 22942 0 None -18 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 22942 0 None -18 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
137661636 166042 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099238 166042 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137662135 166129 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4100231 166129 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44579779 193674 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 COCC(NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C)c1ccccc1 10.1016/j.bmcl.2008.08.039
CHEMBL489787 193674 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 COCC(NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C)c1ccccc1 10.1016/j.bmcl.2008.08.039
15986755 190897 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL482698 190897 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
16125020 144396 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 230 1 1 3 1.4 O=C(O)C1=CC(=O)C2(CCc3ccccc32)O1 10.1021/jm070022x
CHEMBL375753 144396 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 230 1 1 3 1.4 O=C(O)C1=CC(=O)C2(CCc3ccccc32)O1 10.1021/jm070022x
57413546 82886 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 222 4 2 3 1.0 CCOC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
CHEMBL2057607 82886 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 222 4 2 3 1.0 CCOC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
137645601 164630 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083723 164630 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
57413542 83251 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 2 2 2 1.4 O=C(O)c1n[nH]c2c1C[C@@H]1[C@H]2[C@@H]1C1CC1 10.1021/jm2010964
CHEMBL2059829 83251 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 2 2 2 1.4 O=C(O)c1n[nH]c2c1C[C@@H]1[C@H]2[C@@H]1C1CC1 10.1021/jm2010964
56950369 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
59343664 82031 0 None 1 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 82031 0 None 1 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
15604637 82035 0 None 1 3 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036955 82035 0 None 1 3 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
117629482 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
117629482 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 9599 140 None -4 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
11379903 91046 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm800896z
CHEMBL221282 91046 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm800896z
11379903 91046 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 91046 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11206816 91682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 222 2 1 3 1.8 CC1(C2=CCCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223706 91682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 222 2 1 3 1.8 CC1(C2=CCCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
136375465 183912 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4633857 183912 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
46889399 13605 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 242 1 2 4 1.4 C1CCC2(C1)[C@H]1Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1083990 13605 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 242 1 2 4 1.4 C1CCC2(C1)[C@H]1Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]12 10.1016/j.bmcl.2010.03.062
28400056 159002 1 None -74 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 208 5 2 3 2.4 CCC(CC)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL396879 159002 1 None -74 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 208 5 2 3 2.4 CCC(CC)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
57398904 76697 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 280 6 1 6 0.9 CCOCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939017 76697 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 280 6 1 6 0.9 CCOCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
135416388 14296 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1087302 14296 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
135416388 14296 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1087302 14296 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
11672811 7788 5 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 10.1016/j.bmcl.2010.03.062
5790 7788 5 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 10.1016/j.bmcl.2010.03.062
CHEMBL1169573 7788 5 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 10.1016/j.bmcl.2010.03.062
11311474 172561 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2ccc(Cl)s2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL424750 172561 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2ccc(Cl)s2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
24741306 173735 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL428724 173735 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44579761 193937 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
CHEMBL492019 193937 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
44441322 154341 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 3 2 3 1.5 CCCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL393086 154341 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 3 2 3 1.5 CCCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
145985690 172222 0 None -17 3 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4239086 172222 0 None -17 3 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
57412211 82891 1 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@@H]21 10.1021/jm2010964
CHEMBL2057617 82891 1 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@@H]21 10.1021/jm2010964
53238781 7814 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
5789 7814 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770358 7814 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
135416392 14209 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 14209 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
24953854 76727 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939047 76727 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
46890539 13812 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084841 13812 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
57412216 82893 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057619 82893 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
59304931 82011 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 1 2 4 0.3 CC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036814 82011 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 1 2 4 0.3 CC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
44441326 156957 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.8 O=C(O)c1[nH]nc2c1SCC2 10.1016/j.bmcl.2007.06.028
CHEMBL395177 156957 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.8 O=C(O)c1[nH]nc2c1SCC2 10.1016/j.bmcl.2007.06.028
16048921 161796 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401470 161796 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
44441302 100130 23 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL245491 100130 23 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.07.101
57413447 83124 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059224 83124 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
57412300 83250 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2059828 83250 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
46890537 13810 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084839 13810 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
59304949 82024 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 1.1 CCCC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036830 82024 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 1.1 CCCC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
137647495 164635 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083762 164635 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11159621 9326 46 None -1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 9326 46 None -1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 9326 46 None -1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 9326 46 None -1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
11159621 9326 46 None -2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 9326 46 None -2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 9326 46 None -2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 9326 46 None -2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
44579648 193745 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 448 7 1 5 5.3 Cc1c(C(=O)NCCOc2ccc(Cl)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490414 193745 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 448 7 1 5 5.3 Cc1c(C(=O)NCCOc2ccc(Cl)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
44580036 193880 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 5 5.8 Cc1c(C(=O)NCCOc2ccc3ccccc3c2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL491439 193880 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 5 5.8 Cc1c(C(=O)NCCOc2ccc3ccccc3c2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
12003791 201608 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 201608 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 201608 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
11390981 143328 1 None - 1 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 248 3 1 4 1.5 COc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL373752 143328 1 None - 1 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 248 3 1 4 1.5 COc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
2761046 155562 125 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1ccnnc1 10.1016/j.bmcl.2007.06.028
CHEMBL394068 155562 125 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1ccnnc1 10.1016/j.bmcl.2007.06.028
46889362 13956 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1C2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085538 13956 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1C2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
145949989 169739 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 169739 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145949989 169739 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 169739 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
46889320 13426 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1083380 13426 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
57390148 76707 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3ccccc3-c3cccc(C#N)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939027 76707 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3ccccc3-c3cccc(C#N)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
42625218 190958 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483140 190958 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
135416388 14296 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1087302 14296 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
9822 152416 133 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL391574 152416 133 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
11436345 6931 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1599 6931 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL424938 6931 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
24741312 96174 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237036 96174 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135416394 9338 52 None -15 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 9338 52 None -15 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 9338 52 None -15 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 9338 52 None -15 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
11183678 91547 1 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2ccsc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223140 91547 1 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2ccsc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11148966 7906 4 None -4 2 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
1598 7906 4 None -4 2 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
CHEMBL436301 7906 4 None -4 2 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
46889336 13836 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1084950 13836 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
24955288 64829 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 270 4 1 4 2.2 CCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672750 64829 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 270 4 1 4 2.2 CCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
46889363 13957 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085539 13957 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
57412302 82883 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
CHEMBL2057604 82883 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
135416392 14209 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 14209 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
46890538 13811 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084840 13811 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
137632012 163435 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4069406 163435 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11413114 144397 0 None 2 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 3 1.4 CC1(C2=CCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375754 144397 0 None 2 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 3 1.4 CC1(C2=CCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
135899325 22965 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 22965 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
44441311 100442 49 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 142 2 3 3 -0.4 O=C(O)c1cc(CO)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL246903 100442 49 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 142 2 3 3 -0.4 O=C(O)c1cc(CO)n[nH]1 10.1016/j.bmcl.2007.06.028
44441320 154340 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 1 2 3 0.7 CC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL393085 154340 2 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 1 2 3 0.7 CC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
12003790 202834 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL560406 202834 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
17688981 154295 46 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 160 1 2 2 1.1 Cc1[nH]nc(C(=O)O)c1Cl 10.1016/j.bmcl.2007.07.101
CHEMBL393062 154295 46 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 160 1 2 2 1.1 Cc1[nH]nc(C(=O)O)c1Cl 10.1016/j.bmcl.2007.07.101
57400599 76723 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 304 5 2 6 0.6 CCc1cc(=O)oc2nc(OCC#CCCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939043 76723 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 304 5 2 6 0.6 CCc1cc(=O)oc2nc(OCC#CCCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
15604644 82017 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 304 4 2 5 1.4 O=c1[nH]c(=O)c2c(CCCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036823 82017 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 304 4 2 5 1.4 O=c1[nH]c(=O)c2c(CCCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
117629482 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
1588 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
1594 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
2835 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
938 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
CHEMBL573 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
DB00627 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
57393656 76700 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 264 4 1 5 1.5 COc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939020 76700 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 264 4 1 5 1.5 COc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
137637662 163020 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4064786 163020 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11817645 91681 1 None 12 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2cc(F)cc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223700 91681 1 None 12 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2cc(F)cc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
42625382 191591 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
CHEMBL485184 191591 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
156012920 184228 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4638809 184228 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
90645412 119192 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 365 6 2 4 3.4 COc1ccc(/C=C/C(=O)NC2=C(C(=O)O)CCCC2)c(Cl)c1OC 10.1016/j.bmc.2014.05.011
CHEMBL3297797 119192 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 365 6 2 4 3.4 COc1ccc(/C=C/C(=O)NC2=C(C(=O)O)CCCC2)c(Cl)c1OC 10.1016/j.bmc.2014.05.011
46890400 14058 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
CHEMBL1086030 14058 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
44433525 154033 24 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 170 2 2 2 1.1 O=C(O)c1n[nH]c(C2CC2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL392859 154033 24 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 170 2 2 2 1.1 O=C(O)c1n[nH]c(C2CC2)c1F 10.1016/j.bmcl.2007.07.101
117629482 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
1588 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
1594 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
2835 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
938 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
CHEMBL573 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
DB00627 9599 140 None -4 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
135800194 96266 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
CHEMBL237248 96266 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
135800194 96266 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237248 96266 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135966934 13614 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084030 13614 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
135800194 96266 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL237248 96266 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11607970 9330 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 10.1021/jm2010964
5785 9330 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 10.1021/jm2010964
CHEMBL2059221 9330 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 10.1021/jm2010964
11646179 191592 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL485185 191592 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
57400595 76706 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccc(C(F)(F)F)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939026 76706 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccc(C(F)(F)F)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
117629482 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 9599 140 None 3 4 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
137653026 165486 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093294 165486 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44351665 123624 26 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 1 2 3 0.1 O=C(O)c1[nH]nc2c1COC2 10.1016/j.bmcl.2007.06.028
CHEMBL338071 123624 26 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 1 2 3 0.1 O=C(O)c1[nH]nc2c1COC2 10.1016/j.bmcl.2007.06.028
11494579 7844 0 None -123 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
5791 7844 0 None -123 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
CHEMBL482768 7844 0 None -123 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
53324022 64825 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 258 2 1 4 1.6 CCc1cc(=O)oc2nc(C(F)Cl)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672745 64825 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 258 2 1 4 1.6 CCc1cc(=O)oc2nc(C(F)Cl)[nH]c(=O)c12 10.1021/ml100251u
117629482 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
90645407 119296 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 356 4 2 3 3.9 O=C(/C=C/c1cc2ccccc2nc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299016 119296 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 356 4 2 3 3.9 O=C(/C=C/c1cc2ccccc2nc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
53324024 64832 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 4 1 4 2.4 CC(C)CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672753 64832 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 4 1 4 2.4 CC(C)CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
145960556 169001 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4163051 169001 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
117629482 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 9599 140 None -4 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
46889342 13955 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 1.1 C/C=C/[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085537 13955 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 1.1 C/C=C/[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
57412400 82894 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2057620 82894 1 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
145960556 169001 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4163051 169001 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
57413541 83249 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059827 83249 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
46890298 13934 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085414 13934 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
15605646 82020 1 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 5 2 4 1.3 CCCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036826 82020 1 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 5 2 4 1.3 CCCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
24953854 76727 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939047 76727 0 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
11218626 91667 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1csc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL223623 91667 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1csc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
156011372 184131 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4637548 184131 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
11557600 174161 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL429495 174161 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
12003699 202833 5 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 242 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1ccccc1)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL560405 202833 5 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 242 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1ccccc1)CC2 10.1016/j.bmcl.2009.06.054
53326591 64814 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 314 5 1 4 2.6 O=c1cc(CCCC2(F)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672645 64814 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 314 5 1 4 2.6 O=c1cc(CCCC2(F)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
15605364 76693 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 262 4 1 5 1.2 CCc1cc(=O)oc2nc(OCC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939013 76693 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 262 4 1 5 1.2 CCc1cc(=O)oc2nc(OCC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11159621 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
5784 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
CHEMBL456145 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
DB05939 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
11159621 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
5784 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
CHEMBL456145 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
DB05939 9326 46 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
46889398 13604 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 1 2 4 0.9 CC1(C)[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083989 13604 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 1 2 4 0.9 CC1(C)[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
117629482 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
117629482 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1588 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1588 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1594 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1594 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
2835 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
2835 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
938 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
938 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
CHEMBL573 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
CHEMBL573 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
DB00627 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
DB00627 9599 140 None 3 4 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
11380943 90234 1 None 20 2 Human 6.5 pEC50 = 6.5 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL219980 90234 1 None 20 2 Human 6.5 pEC50 = 6.5 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
135416391 13692 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084393 13692 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
135416393 14401 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1088213 14401 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
57400594 76705 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3cccc(C(F)(F)F)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939025 76705 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3cccc(C(F)(F)F)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
136000579 68174 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770175 68174 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
59304795 82008 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 194 0 2 4 -0.5 Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036811 82008 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 194 0 2 4 -0.5 Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
156017210 184509 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
CHEMBL4642367 184509 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
78346 100525 133 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cncnc1 10.1016/j.bmcl.2007.06.028
CHEMBL247316 100525 133 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cncnc1 10.1016/j.bmcl.2007.06.028
57402398 76709 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 394 5 1 7 2.6 CCc1cc(=O)oc2nc(OCc3ccc(-c4cncnc4)cc3F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939029 76709 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 394 5 1 7 2.6 CCc1cc(=O)oc2nc(OCc3ccc(-c4cncnc4)cc3F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
3159638 168690 61 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.0 CCc1[nH]nc(C(=O)O)c1C 10.1016/j.bmcl.2007.07.101
CHEMBL415261 168690 61 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.0 CCc1[nH]nc(C(=O)O)c1C 10.1016/j.bmcl.2007.07.101
136000718 68176 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770177 68176 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
137655320 165317 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091501 165317 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
59343664 82031 0 None -1 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 82031 0 None -1 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
51346919 64617 6 None 1 4 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 64617 6 None 1 4 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
46890270 14147 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086354 14147 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
145949989 169739 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 169739 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145949989 169739 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 169739 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
44579763 193762 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490600 193762 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
24955642 64831 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 6 1 4 2.9 CCCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672752 64831 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 6 1 4 2.9 CCCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
46890297 13986 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085653 13986 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
15605287 82007 2 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 208 1 2 4 -0.3 CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036810 82007 2 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 208 1 2 4 -0.3 CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
70686047 82028 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CCC(C)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036947 82028 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CCC(C)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
53324033 64807 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(COc3ccccc3)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672638 64807 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(COc3ccccc3)[nH]c(=O)c12 10.1021/ml100251u
57412214 82889 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2057615 82889 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
53317467 64813 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 372 6 1 4 3.9 O=c1cc(CCCC2(c3ccccc3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672643 64813 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 372 6 1 4 3.9 O=c1cc(CCCC2(c3ccccc3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57390149 76721 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 276 3 2 6 -0.2 CCc1cc(=O)oc2nc(OCC#CCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939041 76721 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 276 3 2 6 -0.2 CCc1cc(=O)oc2nc(OCC#CCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57390147 76699 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 1 5 2.0 COc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939019 76699 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 1 5 2.0 COc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
136375437 184860 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647670 184860 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
44580007 193726 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
CHEMBL490215 193726 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
54587625 68170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770171 68170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
53318746 64810 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 6 1 4 3.3 CCC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672640 64810 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 6 1 4 3.3 CCC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
16048919 101458 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
CHEMBL252708 101458 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
11470032 91523 1 None - 1 Human 4.5 pEC50 = 4.5 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 219 2 1 4 0.9 CC1(c2cccnc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222949 91523 1 None - 1 Human 4.5 pEC50 = 4.5 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 219 2 1 4 0.9 CC1(c2cccnc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
53326616 64824 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 2 1 4 0.9 CCc1cc(=O)oc2nc(CF)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672744 64824 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 2 1 4 0.9 CCc1cc(=O)oc2nc(CF)[nH]c(=O)c12 10.1021/ml100251u
137659759 166046 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099278 166046 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
53325309 64836 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 236 3 1 5 0.6 CCc1cc(=O)oc2nc(COC)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672768 64836 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 236 3 1 5 0.6 CCc1cc(=O)oc2nc(COC)[nH]c(=O)c12 10.1021/ml100251u
11516324 190995 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483352 190995 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
57398906 76719 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 286 3 1 5 1.2 CCc1cc(=O)oc2nc(OCC#CC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939039 76719 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 286 3 1 5 1.2 CCc1cc(=O)oc2nc(OCC#CC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11493732 199879 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL522649 199879 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
135899178 22982 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 22982 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
11610260 152727 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 364 6 2 4 4.2 Cc1noc(C)c1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
CHEMBL391812 152727 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 364 6 2 4 4.2 Cc1noc(C)c1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
136088957 68177 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770178 68177 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
44433534 159190 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 210 4 2 4 1.1 CCCCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL397056 159190 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 210 4 2 4 1.1 CCCCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
28400046 96585 3 None -32 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 1.8 CC(C)CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237737 96585 3 None -32 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 1.8 CC(C)CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
53318768 64823 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 242 2 1 4 1.4 CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672743 64823 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 242 2 1 4 1.4 CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
136088958 68220 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770353 68220 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
137639493 163690 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4072283 163690 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
90645405 119310 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299113 119310 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
90645414 119198 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 338 5 2 3 3.5 Cc1ccc2cc(CCC(=O)NC3=C(C(=O)O)CCCC3)ccc2n1 10.1016/j.bmc.2014.05.011
CHEMBL3297874 119198 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 338 5 2 3 3.5 Cc1ccc2cc(CCC(=O)NC3=C(C(=O)O)CCCC3)ccc2n1 10.1016/j.bmc.2014.05.011
57413367 82888 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057614 82888 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
11436345 6931 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1599 6931 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL424938 6931 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
11446592 156612 3 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 172 3 2 3 1.0 CSCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL394885 156612 3 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 172 3 2 3 1.0 CSCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
46889364 14010 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 4 2 4 1.7 CCCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085760 14010 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 4 2 4 1.7 CCCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
53317492 64819 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.8 CC1CC(CCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)C1 10.1021/ml100251u
CHEMBL1672737 64819 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.8 CC1CC(CCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)C1 10.1021/ml100251u
56659539 70592 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 337 5 3 4 3.3 O=C(COc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm200371q
CHEMBL1802361 70592 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 337 5 3 4 3.3 O=C(COc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm200371q
11493732 199879 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL522649 199879 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
12002802 202612 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
CHEMBL558334 202612 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
136088960 68222 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1770355 68222 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
59304954 82036 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036956 82036 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
117629482 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
117629482 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1588 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1588 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1594 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1594 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
2835 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
2835 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
938 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
938 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
CHEMBL573 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
CHEMBL573 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
DB00627 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
DB00627 9599 140 None -3 4 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
137654580 165801 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4096635 165801 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
676464 96651 75 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL237788 96651 75 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
15604642 82029 0 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036948 82029 0 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
15604637 82035 0 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036955 82035 0 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
51346919 64617 6 None -1 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 64617 6 None -1 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
59304608 82034 0 None -3 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 82034 0 None -3 4 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
15604642 82029 0 None -1 3 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036948 82029 0 None -1 3 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11501698 199349 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL521326 199349 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
1597 8746 80 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm800896z
2736690 8746 80 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm800896z
CHEMBL381638 8746 80 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm800896z
11159621 9326 46 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 9326 46 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 9326 46 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 9326 46 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
11693991 95310 1 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 2 2 4 0.7 CC(C)c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL235229 95310 1 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 2 2 4 0.7 CC(C)c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
24180571 96704 26 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 144 1 2 2 0.6 Cc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL238004 96704 26 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 144 1 2 2 0.6 Cc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
24811199 13373 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083139 13373 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
54584718 68225 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770359 68225 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
137650474 164058 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4076822 164058 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
90645406 119199 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 388 6 2 4 3.9 COc1ccc2nc(Cl)c(CCC(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
CHEMBL3297875 119199 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 388 6 2 4 3.9 COc1ccc2nc(Cl)c(CCC(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
90645404 119295 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 322 4 2 3 3.3 O=C(/C=C/c1ccc2ccccc2n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299009 119295 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 322 4 2 3 3.3 O=C(/C=C/c1ccc2ccccc2n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
11323649 91524 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.8 CC1(c2cc(Cl)ccc2Cl)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222955 91524 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.8 CC1(c2cc(Cl)ccc2Cl)OC(C(=O)O)=CC1=O 10.1021/jm070022x
53321368 64833 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 4 1 4 3.3 O=c1cc(CCC2CCCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672754 64833 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 4 1 4 3.3 O=c1cc(CCC2CCCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57402397 76698 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 250 4 1 5 1.2 CCCCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939018 76698 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 250 4 1 5 1.2 CCCCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
136086829 14110 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
CHEMBL1086225 14110 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
11219885 90237 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.5 CC1(c2cccc(C(F)(F)F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL220001 90237 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.5 CC1(c2cccc(C(F)(F)F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
57397203 76730 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 4 1 5 1.2 CC#CCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939050 76730 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 4 1 5 1.2 CC#CCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
15605359 76716 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 260 3 1 5 0.8 CC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939036 76716 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 260 3 1 5 0.8 CC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
42625475 190988 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483336 190988 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
57412216 82893 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057619 82893 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
11739420 91532 0 None 12 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 344 2 1 3 2.1 CC1(c2cccc(I)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223013 91532 0 None 12 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 344 2 1 3 2.1 CC1(c2cccc(I)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
135800176 96175 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237037 96175 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890268 13378 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1083174 13378 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
44433526 95265 18 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 246 4 2 2 2.2 CCCCc1[nH]nc(C(=O)O)c1Br 10.1016/j.bmcl.2007.07.101
CHEMBL235010 95265 18 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 246 4 2 2 2.2 CCCCc1[nH]nc(C(=O)O)c1Br 10.1016/j.bmcl.2007.07.101
16048768 101225 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
CHEMBL251222 101225 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
12003785 203158 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL562632 203158 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
53318741 64828 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 256 3 1 4 1.8 CCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672749 64828 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 256 3 1 4 1.8 CCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
46889319 13902 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 C1c2c(-c3nnn[nH]3)n[nH]c2[C@H]2C[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085289 13902 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 C1c2c(-c3nnn[nH]3)n[nH]c2[C@H]2C[C@@H]12 10.1016/j.bmcl.2010.03.062
11560300 95314 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235256 95314 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890577 13444 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083442 13444 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
137640776 163783 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073322 163783 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
90645403 119257 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 321 4 2 2 3.9 O=C(/C=C/c1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298700 119257 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 321 4 2 2 3.9 O=C(/C=C/c1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
12003791 201608 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 201608 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 201608 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
24955294 64816 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 4 1 4 2.2 O=c1cc(CCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672733 64816 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 4 1 4 2.2 O=c1cc(CCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
145957123 168796 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4159670 168796 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
145957123 168796 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4159670 168796 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
46890578 13163 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1082294 13163 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
44579647 199800 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccc(F)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL522281 199800 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccc(F)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
9822 152416 133 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL391574 152416 133 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
46890501 14018 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085816 14018 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
16048840 100819 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL248851 100819 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
135416394 9338 52 None -288 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 9338 52 None -288 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 9338 52 None -288 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 9338 52 None -288 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
11367769 143342 1 None - 1 Human 4.3 pEC50 = 4.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 4 1.1 CC1(c2ccco2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL373880 143342 1 None - 1 Human 4.3 pEC50 = 4.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 4 1.1 CC1(c2ccco2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11379903 91046 0 None 6 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 91046 0 None 6 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
59304594 82018 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 5 1.0 O=c1[nH]c(=O)c2c(CCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036824 82018 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 5 1.0 O=c1[nH]c(=O)c2c(CCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
135401973 7809 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
5792 7809 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL398496 7809 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
53322689 64834 1 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1672755 64834 1 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
59304859 82023 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 300 4 2 6 -0.9 CS(=O)(=O)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036829 82023 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 300 4 2 6 -0.9 CS(=O)(=O)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
53322689 64834 1 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672755 64834 1 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1021/ml100251u
53321396 64818 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 O=c1cc(CCCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672736 64818 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 O=c1cc(CCCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
11483496 6914 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1589 6914 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL375493 6914 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
42625476 190989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483337 190989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
11276453 91651 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1ccc(C2(C)OC(C(=O)O)=CC2=O)s1 10.1021/jm070022x
CHEMBL223566 91651 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1ccc(C2(C)OC(C(=O)O)=CC2=O)s1 10.1021/jm070022x
46890399 14057 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086029 14057 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
156013148 184247 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4639053 184247 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
24955646 64808 0 None -8 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 64808 0 None -8 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
46890500 14017 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085815 14017 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
44441305 156900 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 188 3 2 3 -0.0 C[S+]([O-])Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL395118 156900 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 188 3 2 3 -0.0 C[S+]([O-])Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
15604641 82030 1 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 4 2 4 1.1 CC(C)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036950 82030 1 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 4 2 4 1.1 CC(C)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
59343664 82031 0 None -2 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 82031 0 None -2 4 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
59304608 82034 0 None -5 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 82034 0 None -5 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
135466520 190996 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483353 190996 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
135899171 22942 0 None 18 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 22942 0 None 18 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
776416 25710 108 None 5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL128604 25710 108 None 5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
11594881 95413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL235740 95413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
98845 100491 125 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 143 1 1 3 1.2 Cc1ncc(C(=O)O)s1 10.1016/j.bmcl.2007.06.028
CHEMBL247134 100491 125 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 143 1 1 3 1.2 Cc1ncc(C(=O)O)s1 10.1016/j.bmcl.2007.06.028
136088959 68221 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770354 68221 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11183677 90238 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2cccs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL220004 90238 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2cccs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
117629482 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1588 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1594 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
2835 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
938 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
CHEMBL573 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
DB00627 9599 140 None -4 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
16048839 161795 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401469 161795 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
46889337 13495 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 2 2 4 0.9 CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083682 13495 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 2 2 4 0.9 CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
46889340 13953 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 0.9 C1CC1[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085535 13953 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 0.9 C1CC1[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
42625379 198870 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520299 198870 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
117629482 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
1588 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
1594 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
2835 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
938 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
CHEMBL573 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
DB00627 9599 140 None -4 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
90645411 119200 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 317 5 2 4 2.4 O=C(CCc1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3297876 119200 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 317 5 2 4 2.4 O=C(CCc1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
1595 7047 49 None 4 2 Human 6.3 pEC50 = 6.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
51576 7047 49 None 4 2 Human 6.3 pEC50 = 6.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
CHEMBL278488 7047 49 None 4 2 Human 6.3 pEC50 = 6.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
117629482 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1588 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1594 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
2835 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
938 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
CHEMBL573 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
DB00627 9599 140 None -4 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
24954935 76718 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 288 4 1 5 1.6 CCCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939038 76718 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 288 4 1 5 1.6 CCCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
1596 7048 96 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
5310993 7048 96 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
76 7048 96 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
CHEMBL345714 7048 96 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
DB09055 7048 96 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
120232 160064 132 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 141 1 1 2 0.9 O=C(O)c1cncc(F)c1 10.1016/j.bmcl.2007.06.028
CHEMBL397783 160064 132 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 141 1 1 2 0.9 O=C(O)c1cncc(F)c1 10.1016/j.bmcl.2007.06.028
46890296 13985 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 364 5 3 4 3.3 N#CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1085652 13985 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 364 5 3 4 3.3 N#CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
57412297 83247 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059822 83247 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
11638560 193822 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491002 193822 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
11345283 91786 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 2 1 3 1.8 Cc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL223878 91786 1 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 2 1 3 1.8 Cc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
11264843 144398 1 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccc(F)cc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375762 144398 1 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccc(F)cc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
46889341 13954 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 230 3 2 4 1.3 CCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085536 13954 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 230 3 2 4 1.3 CCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
57412218 83125 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2059225 83125 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
52941721 61739 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1204125 61739 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1615577 61739 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
44441323 100608 10 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.9 O=C(O)c1[nH]nc2c1CSC2 10.1016/j.bmcl.2007.06.028
CHEMBL247724 100608 10 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.9 O=C(O)c1[nH]nc2c1CSC2 10.1016/j.bmcl.2007.06.028
44441312 100639 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 6 2 2 2.2 CCCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL247922 100639 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 6 2 2 2.2 CCCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
137648318 164411 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4081260 164411 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44433524 158987 29 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 158 2 2 2 0.8 CCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL396864 158987 29 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 158 2 2 2 0.8 CCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
11380943 90234 1 None 20 2 Human 6.2 pEC50 = 6.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL219980 90234 1 None 20 2 Human 6.2 pEC50 = 6.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11368347 91721 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223754 91721 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
57412214 82889 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2057615 82889 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
135401975 101523 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL253128 101523 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
90645410 119311 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 315 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299114 119311 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 315 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
57391931 76713 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 345 6 1 7 2.1 CCc1noc(CC)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939033 76713 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 345 6 1 7 2.1 CCc1noc(CC)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
44433533 95965 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 194 2 2 4 0.6 Fc1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
CHEMBL236728 95965 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 194 2 2 4 0.6 Fc1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
51346919 64617 6 None -19 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 64617 6 None -19 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
11617151 95414 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235741 95414 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11617151 95414 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL235741 95414 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm900151e
16048998 101407 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252307 101407 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
53324057 64821 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 6 1 4 2.9 O=c1cc(CCCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672741 64821 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 6 1 4 2.9 O=c1cc(CCCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
135453098 95509 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL236162 95509 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
136086828 13965 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1085589 13965 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
135453098 95509 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL236162 95509 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
56950369 10332 13 None -3 4 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 10332 13 None -3 4 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 10332 13 None -3 4 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 10332 13 None -3 4 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
24955646 64808 0 None 2 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 64808 0 None 2 4 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
42625474 190957 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483139 190957 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
11624691 13999 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1085711 13999 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
136127010 22858 11 None 9 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 22858 11 None 9 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
882926 92382 13 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
CHEMBL228244 92382 13 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
882926 92382 13 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm900151e
CHEMBL228244 92382 13 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm900151e
44580008 193727 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490216 193727 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
53318740 64826 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 238 2 1 4 1.5 CCc1cc(=O)oc2nc(C(C)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672746 64826 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 238 2 1 4 1.5 CCc1cc(=O)oc2nc(C(C)F)[nH]c(=O)c12 10.1021/ml100251u
11322762 144380 1 None 5 2 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2c(F)cccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375625 144380 1 None 5 2 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2c(F)cccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
17925840 100396 17 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 3 -0.1 O=Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL246692 100396 17 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 3 -0.1 O=Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
70683894 82016 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 298 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCc3ccccc3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036822 82016 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 298 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCc3ccccc3)cc(=O)oc2[nH]1 10.1021/ml200243g
15986930 191689 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485327 191689 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
11776293 156036 8 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL394441 156036 8 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1016/j.bmcl.2007.06.028
56950649 76712 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 331 5 1 7 1.9 CCc1noc(C)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939032 76712 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 331 5 1 7 1.9 CCc1noc(C)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
137653428 165322 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091542 165322 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44445341 161027 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL398625 161027 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
90645409 119309 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 386 5 2 4 3.9 COc1ccc2nc(Cl)c(/C=C/C(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
CHEMBL3299112 119309 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 386 5 2 4 3.9 COc1ccc2nc(Cl)c(/C=C/C(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
1047 209415 130 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cnccn1 10.1016/j.bmcl.2007.06.028
CHEMBL613 209415 130 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cnccn1 10.1016/j.bmcl.2007.06.028
11494579 7844 0 None 123 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
5791 7844 0 None 123 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
CHEMBL482768 7844 0 None 123 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
24811550 13452 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083450 13452 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
156021045 184910 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4648435 184910 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
135887289 13693 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084394 13693 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
54580748 68172 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770173 68172 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
53321367 64827 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 228 1 1 4 1.1 Cc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672748 64827 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 228 1 1 4 1.1 Cc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
11379903 91046 0 None 6 2 Human 7.2 pEC50 = 7.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 91046 0 None 6 2 Human 7.2 pEC50 = 7.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
24953855 76725 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 316 5 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939045 76725 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 316 5 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
44441316 100565 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 194 3 2 2 1.9 CCCC1CCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL247526 100565 1 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 194 3 2 2 1.9 CCCC1CCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
24953853 76729 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939049 76729 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
117629482 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1588 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1594 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
2835 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
938 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
CHEMBL573 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
DB00627 9599 140 None -3 4 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
90645408 119312 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 329 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299115 119312 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 329 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
42625213 199082 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520620 199082 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
59343597 82040 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 296 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3(Cl)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036960 82040 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 296 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3(Cl)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
57412301 82881 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
CHEMBL2057602 82881 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
122181142 128608 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3589836 128608 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44579762 193938 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL492020 193938 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
11415838 143135 0 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 316 2 1 4 2.6 Cc1sc(C2(C)OC(C(=O)O)=CC2=O)cc1Br 10.1021/jm070022x
CHEMBL373484 143135 0 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 316 2 1 4 2.6 Cc1sc(C2(C)OC(C(=O)O)=CC2=O)cc1Br 10.1021/jm070022x
137661033 166266 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4101720 166266 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11470798 144745 1 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)c(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL376419 144745 1 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)c(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
156020475 184853 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
CHEMBL4647545 184853 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
136088961 68224 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770357 68224 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
57397202 76708 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3cccc(-c4cccc(C#N)c4)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939028 76708 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3cccc(-c4cccc(C#N)c4)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
135887288 14388 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
CHEMBL1088074 14388 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
135922719 191066 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
CHEMBL483996 191066 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
15605503 76710 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 299 4 1 6 1.4 CCc1cc(=O)oc2nc(OCc3cccnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939030 76710 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 299 4 1 6 1.4 CCc1cc(=O)oc2nc(OCc3cccnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
135502978 198768 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520136 198768 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
11324121 91441 0 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 CC1(c2cc(Br)cs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222472 91441 0 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 CC1(c2cc(Br)cs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
46890579 13788 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084798 13788 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
46890580 13789 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1084799 13789 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
44433532 159188 0 None 16 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 2 2 4 0.3 CCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL397055 159188 0 None 16 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 2 2 4 0.3 CCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
15986931 199015 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL520513 199015 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
15986755 190897 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL482698 190897 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
156021546 184965 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649305 184965 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
247986 156959 129 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 157 1 1 2 1.4 O=C(O)c1cncc(Cl)c1 10.1016/j.bmcl.2007.06.028
CHEMBL395178 156959 129 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 157 1 1 2 1.4 O=C(O)c1cncc(Cl)c1 10.1016/j.bmcl.2007.06.028
11647028 95457 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235954 95457 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
574310 25728 148 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL128679 25728 148 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1016/j.bmcl.2007.07.101
44433528 154300 0 None -10 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 3 2 4 0.5 CCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393064 154300 0 None -10 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 3 2 4 0.5 CCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
117629482 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
1588 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
1594 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
2835 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
938 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
CHEMBL573 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
DB00627 9599 140 None -4 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
16048993 175756 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2ncc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL439060 175756 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2ncc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
53324034 64811 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 338 6 1 4 3.6 CC(C)C1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672641 64811 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 338 6 1 4 3.6 CC(C)C1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
10197980 95264 2 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 186 4 2 2 1.6 CCCCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL235009 95264 2 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 186 4 2 2 1.6 CCCCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
4913402 156101 74 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL394498 156101 74 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
16048845 173954 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 420 4 3 6 1.8 NC(=O)c1ccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc2c1 10.1016/j.bmcl.2007.10.055
CHEMBL429120 173954 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 420 4 3 6 1.8 NC(=O)c1ccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc2c1 10.1016/j.bmcl.2007.10.055
56950369 10332 13 None -3 4 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 10332 13 None -3 4 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 10332 13 None -3 4 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 10332 13 None -3 4 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
15605571 82010 2 None 1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 82010 2 None 1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
117629482 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
1588 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
1594 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
2835 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
938 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
CHEMBL573 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
DB00627 9599 140 None -4 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
137635425 162701 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4060899 162701 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
4913402 156101 74 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL394498 156101 74 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
57413450 83246 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059821 83246 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
156022048 184980 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649587 184980 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
53317491 64817 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 3 1 4 2.2 O=c1cc(CC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672735 64817 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 3 1 4 2.2 O=c1cc(CC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57413545 82884 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
CHEMBL2057605 82884 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
24953853 76729 0 None -1 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939049 76729 0 None -1 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
11845295 156357 42 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
CHEMBL394688 156357 42 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
15986754 191269 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 323 5 2 2 3.8 O=C(CCc1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL484719 191269 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 323 5 2 2 3.8 O=C(CCc1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
776421 96703 108 None 30 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL238002 96703 108 None 30 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
11845295 156357 42 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1016/j.bmcl.2007.06.028
CHEMBL394688 156357 42 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1016/j.bmcl.2007.06.028
135922722 190970 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
CHEMBL483160 190970 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
57412301 82881 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
CHEMBL2057602 82881 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
136000580 68223 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770356 68223 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
1591 6919 63 None 33 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
6485181 6919 63 None 33 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
CHEMBL428730 6919 63 None 33 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
57412303 82885 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
CHEMBL2057606 82885 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
11617480 95456 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235952 95456 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
776416 25710 108 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL128604 25710 108 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
57398905 76702 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3cccc(OC)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939022 76702 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3cccc(OC)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
776416 25710 108 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2007.06.028
CHEMBL128604 25710 108 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2007.06.028
44441304 100193 20 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 156 3 2 3 0.3 COCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL245858 100193 20 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 156 3 2 3 0.3 COCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
44441321 100607 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 2 2 3 1.1 CCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL247723 100607 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 2 2 3 1.1 CCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
136088962 68175 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770176 68175 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11041813 100526 22 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL247317 100526 22 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1016/j.bmcl.2007.06.028
137648386 164551 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4082765 164551 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
24954201 76728 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 314 5 1 5 2.0 CCC#CCOc1nc2oc(=O)cc(CCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939048 76728 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 314 5 1 5 2.0 CCC#CCOc1nc2oc(=O)cc(CCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
90645402 119259 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 2 3 3 2.9 O=C(C#Cc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298702 119259 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 2 3 3 2.9 O=C(C#Cc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
16048923 101431 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252506 101431 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
15981408 101121 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL250690 101121 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
57391932 76715 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 246 3 1 5 0.5 C#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939035 76715 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 246 3 1 5 0.5 C#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
44250176 7915 0 None -2951 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
5800 7915 0 None -2951 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
CHEMBL564300 7915 0 None -2951 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
24811547 14148 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086355 14148 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
24741307 95510 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
CHEMBL236163 95510 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
57400596 76711 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 300 4 1 7 0.8 CCc1cc(=O)oc2nc(OCc3ccnnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939031 76711 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 300 4 1 7 0.8 CCc1cc(=O)oc2nc(OCc3ccnnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11610363 96265 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237247 96265 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44579645 193847 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
CHEMBL491227 193847 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
135627640 68171 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770172 68171 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
15605292 82013 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 266 3 2 6 -0.7 CCOC(=O)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036819 82013 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 266 3 2 6 -0.7 CCOC(=O)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11992789 203377 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 343 6 2 3 3.6 O=C(O)c1cc(N(Cc2cccc(F)c2)Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL564064 203377 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 343 6 2 3 3.6 O=C(O)c1cc(N(Cc2cccc(F)c2)Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2009.05.108
46890328 13453 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083451 13453 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
44579742 193823 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491003 193823 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
136375455 184333 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4640349 184333 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
57395377 76717 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 3 1 5 1.2 CCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939037 76717 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 3 1 5 1.2 CCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
11566404 152449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391603 152449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
136086824 13615 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084031 13615 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
117629482 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1588 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1594 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
2835 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
938 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
CHEMBL573 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
DB00627 9599 140 None -4 4 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
59304624 82009 2 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 2 2 4 0.1 CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036812 82009 2 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 2 2 4 0.1 CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
853085 154776 111 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 127 1 1 3 0.7 Cc1cc(C(=O)O)on1 10.1074/jbc.m701866200
CHEMBL393428 154776 111 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 127 1 1 3 0.7 Cc1cc(C(=O)O)on1 10.1074/jbc.m701866200
11550911 101963 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1074/jbc.m701866200
CHEMBL255877 101963 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1074/jbc.m701866200
11557600 174161 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1074/jbc.m701866200
CHEMBL429495 174161 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1074/jbc.m701866200
776421 96703 108 None 30 2 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
CHEMBL238002 96703 108 None 30 2 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
11776293 156036 8 None - 1 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1074/jbc.m701866200
CHEMBL394441 156036 8 None - 1 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1074/jbc.m701866200
1595 7047 49 None 4 2 Human 6.3 pIC50 = 6.3 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
51576 7047 49 None 4 2 Human 6.3 pIC50 = 6.3 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
CHEMBL278488 7047 49 None 4 2 Human 6.3 pIC50 = 6.3 Functional
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
117629482 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1588 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1594 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
2835 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
938 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
CHEMBL573 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
DB00627 9599 140 None -4 4 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
108 6899 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
1590 6899 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
3505 6899 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
CHEMBL1741437 6899 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
1596 7048 96 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
5310993 7048 96 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
76 7048 96 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
CHEMBL345714 7048 96 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
DB09055 7048 96 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
1059 7537 81 None -67 3 Human 2.8 pEC50 = 2.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
264 7537 81 None -67 3 Human 2.8 pEC50 = 2.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
CHEMBL14227 7537 81 None -67 3 Human 2.8 pEC50 = 2.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
DB03568 7537 81 None -67 3 Human 2.8 pEC50 = 2.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
1593 7396 0 None -2 2 Human 3.1 pEC50 = 3.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
92135 7396 0 None -2 2 Human 3.1 pEC50 = 3.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
CHEMBL1162484 7396 0 None -2 2 Human 3.1 pEC50 = 3.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
5787 9779 119 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
637542 9779 119 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
CHEMBL66879 9779 119 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
DB04066 9779 119 None - 1 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
3203 7726 111 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 19136666
444539 7726 111 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 19136666
CHEMBL27246 7726 111 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 19136666
5369209 9369 81 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
5786 9369 81 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
CHEMBL589586 9369 81 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
DB14219 9369 81 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
1596 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
1596 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
5310993 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
5310993 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
76 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
76 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
CHEMBL345714 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
CHEMBL345714 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
DB09055 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
DB09055 7048 96 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
5794 7882 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 5 4.3 ClC1CCC(CC1Cl)c1cnn2c1ncc(c2C)C(=O)NCCOc1ccccc1 22420767
73755156 7882 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 5 4.3 ClC1CCC(CC1Cl)c1cnn2c1ncc(c2C)C(=O)NCCOc1ccccc1 22420767
11159621 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
5784 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
CHEMBL456145 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
DB05939 9326 46 None -1 3 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
117629482 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
117629482 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
117629482 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1588 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1588 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1588 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1594 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1594 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1594 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
2835 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
2835 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
2835 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
938 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
938 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
938 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
CHEMBL573 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
CHEMBL573 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
CHEMBL573 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
DB00627 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
DB00627 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
DB00627 9599 140 None -4 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
25101223 7935 7 None - 1 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 18752940
5795 7935 7 None - 1 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 18752940
CHEMBL490599 7935 7 None - 1 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 18752940
11672811 7788 5 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 20363624
5790 7788 5 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 20363624
CHEMBL1169573 7788 5 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 20363624
46215799 8661 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 4 2 4 1.3 CCCCCn1c(=O)[nH]c(=O)c2c1nc([nH]2)Cl 25773497
8470 8661 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 4 2 4 1.3 CCCCCn1c(=O)[nH]c(=O)c2c1nc([nH]2)Cl 25773497
CHEMBL3730241 8661 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 4 2 4 1.3 CCCCCn1c(=O)[nH]c(=O)c2c1nc([nH]2)Cl 25773497
11607970 9330 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 22435740
5785 9330 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 22435740
CHEMBL2059221 9330 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 22435740
135416394 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
5788 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
73755154 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
CHEMBL1086657 9338 52 None 15 3 Human 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
56950369 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
8469 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
CHEMBL2036958 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
DB12433 10332 13 None 3 4 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
1593 7396 0 None 2 2 Mouse 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
92135 7396 0 None 2 2 Mouse 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
CHEMBL1162484 7396 0 None 2 2 Mouse 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
1592 6932 131 None - 1 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 12522134
256208 6932 131 None - 1 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 12522134
CHEMBL247132 6932 131 None - 1 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 12522134
108 6899 0 None - 1 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
1590 6899 0 None - 1 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
3505 6899 0 None - 1 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
CHEMBL1741437 6899 0 None - 1 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
1595 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
1595 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
1595 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
1595 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
51576 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
51576 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
51576 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
51576 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
CHEMBL278488 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
CHEMBL278488 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
CHEMBL278488 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
CHEMBL278488 7047 49 None 4 2 Human 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
11483496 6914 0 None 14 2 Human 7.3 pEC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 15929991
11483496 6914 0 None 14 2 Human 7.3 pEC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
1589 6914 0 None 14 2 Human 7.3 pEC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 15929991
1589 6914 0 None 14 2 Human 7.3 pEC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
CHEMBL375493 6914 0 None 14 2 Human 7.3 pEC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 15929991
CHEMBL375493 6914 0 None 14 2 Human 7.3 pEC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
53232 195404 95 None -1 10 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 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 None
CHEMBL503 195404 95 None -1 10 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 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 None
12003694 7927 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 20615702
5793 7927 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 20615702
CHEMBL1208986 7927 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 20615702
135401973 7809 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 18029181
5792 7809 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 18029181
CHEMBL398496 7809 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 18029181
11494579 7844 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 19309152
5791 7844 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 19309152
CHEMBL482768 7844 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 19309152
53238781 7814 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 21185185
5789 7814 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 21185185
CHEMBL1770358 7814 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 21185185




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

1596 7048 96 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
5310993 7048 96 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
76 7048 96 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL345714 7048 96 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
DB09055 7048 96 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
117629482 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1588 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1594 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
2835 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
938 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
CHEMBL573 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
DB00627 9599 140 None -3 2 Human 6.0 pEC50 = 6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
11516424 14087 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1086104 14087 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
11625092 13456 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1083473 13456 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
156017170 184427 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 417 5 1 6 4.4 CCOc1cc(Cl)c(C(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4641449 184427 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 417 5 1 6 4.4 CCOc1cc(Cl)c(C(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
57422810 184440 4 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641579 184440 4 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
46890275 13302 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082823 13302 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
24741310 96397 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL237543 96397 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
117629482 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1588 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1594 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
2835 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
938 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
CHEMBL573 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
DB00627 9599 140 None -3 2 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
156021885 184994 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649741 184994 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
1595 7047 49 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
51576 7047 49 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
CHEMBL278488 7047 49 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
156018500 184703 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 629 7 1 10 4.5 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4645314 184703 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 629 7 1 10 4.5 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156019324 184753 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 7 1 8 4.9 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4646005 184753 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 7 1 8 4.9 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
46890274 13678 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1084332 13678 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
46890273 13621 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1084060 13621 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
156011618 184177 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 544 7 1 8 3.6 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)COC)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4638263 184177 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 544 7 1 8 3.6 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)COC)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
15986936 13873 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085150 13873 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
11197 7852 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
154699458 7852 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL4632411 7852 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
46890276 13303 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082824 13303 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
46890240 13875 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085156 13875 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
46890237 13871 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085148 13871 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
46890199 13930 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085401 13930 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
156016073 184434 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4641503 184434 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
46890165 14086 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086103 14086 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
15986929 13931 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1085402 13931 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
156016110 184477 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642043 184477 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
46890272 13619 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084059 13619 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
46890164 14194 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086568 14194 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
11560300 95314 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL235256 95314 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
117629482 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1588 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1594 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
2835 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
938 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
CHEMBL573 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
DB00627 9599 140 None -3 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
53322689 64834 1 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL1672755 64834 1 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1039/d2md00076h
15605571 82010 2 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL2036813 82010 2 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5270112 200399 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 252 3 2 4 1.9 CCCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5275861 200651 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 286 4 2 4 2.1 O=c1cc(CCCCCl)c2c(=O)[nH]c(=S)[nH]c2o1 10.1039/d2md00076h
CHEMBL5277000 200700 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 238 2 2 4 1.5 CCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5281556 200895 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 210 0 2 4 0.8 Cc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5284951 201052 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 270 4 2 4 0.7 O=c1[nH]c(=O)c2c(CCCCCl)cc(=O)oc2[nH]1 10.1039/d2md00076h
46890239 13706 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084448 13706 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
117629482 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1588 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1594 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
2835 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
938 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
CHEMBL573 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
DB00627 9599 140 None -3 2 Human 6.2 pEC50 = 6.2 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
156021336 184946 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4649089 184946 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
46890301 13971 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085616 13971 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
156012428 184089 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4636832 184089 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
46890300 14187 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1086541 14187 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
46890198 14089 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1086108 14089 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
46890238 13872 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085149 13872 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
9822 152416 133 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
CHEMBL391574 152416 133 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
156014693 183971 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4635089 183971 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
24741307 95510 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL236163 95510 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
46890197 14031 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1085875 14031 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
46890302 14024 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1085842 14024 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
46890163 14193 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086567 14193 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
135453098 95509 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL236162 95509 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
42625475 190988 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483336 190988 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
42625476 190989 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483337 190989 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
136000619 68219 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770352 68219 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
135453098 95509 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL236162 95509 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
46890272 13619 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084059 13619 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
135800177 152729 7 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 152729 7 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135800177 152729 7 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL391813 152729 7 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
135627640 68171 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770172 68171 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
136088959 68221 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770354 68221 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
44580008 193727 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490216 193727 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
156013291 184284 0 None - 0 Human 4.0 pIC50 = 4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 455 9 3 9 1.8 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCN2CCOCC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4639589 184284 0 None - 0 Human 4.0 pIC50 = 4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 455 9 3 9 1.8 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCN2CCOCC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
122181143 128609 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 367 6 3 4 4.4 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1sccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589837 128609 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 367 6 3 4 4.4 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1sccc1C(=O)O 10.1016/j.bmc.2015.02.018
122181142 128608 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2015.02.018
CHEMBL3589836 128608 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2015.02.018
136000718 68176 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770177 68176 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
11617852 191314 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL484783 191314 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890297 13986 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085653 13986 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
136000580 68223 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770356 68223 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
15981408 101121 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL250690 101121 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
156011372 184131 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4637548 184131 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
49862074 21746 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208921 21746 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
135899129 22910 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223961 22910 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156012920 184228 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4638809 184228 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
44591603 198481 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519689 198481 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
136000669 68178 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770179 68178 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
46890276 13303 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082824 13303 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
136086828 13965 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1085589 13965 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
53238781 7814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
5789 7814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770358 7814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
11566404 152449 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391603 152449 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890400 14058 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
CHEMBL1086030 14058 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
54585613 68173 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770174 68173 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
16048839 161795 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401469 161795 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
4268702 176431 8 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
CHEMBL443733 176431 8 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
11159621 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
5784 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
CHEMBL456145 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
DB05939 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
11159621 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
5784 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
CHEMBL456145 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
DB05939 9326 46 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
135899108 22983 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224220 22983 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
122181139 128605 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(O)ccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
CHEMBL3589833 128605 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(O)ccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
11494579 7844 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
5791 7844 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
CHEMBL482768 7844 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
135416383 191688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485326 191688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
54580748 68172 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770173 68172 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
137635325 162928 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4063682 162928 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
135922722 190970 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
CHEMBL483160 190970 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
135899320 22905 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 297 6 1 5 2.2 O=c1[nH]c(OCCCOc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223957 22905 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 297 6 1 5 2.2 O=c1[nH]c(OCCCOc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
44579762 193938 1 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL492020 193938 1 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
49862074 21746 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208921 21746 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
11183317 198249 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL519338 198249 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
136127010 22858 11 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 22858 11 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890273 13621 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1084060 13621 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
137655320 165317 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091501 165317 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890274 13678 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1084332 13678 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
46890399 14057 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086029 14057 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
135401973 7809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
5792 7809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL398496 7809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
11594881 95413 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235740 95413 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
117629482 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
11594881 95413 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL235740 95413 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
12002517 198661 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519966 198661 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002525 199122 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
CHEMBL520676 199122 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
117629482 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1588 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1594 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
2835 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
938 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
CHEMBL573 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
DB00627 9599 140 None -3 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
117629482 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1588 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1594 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
2835 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
938 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
CHEMBL573 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
DB00627 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
12002522 195235 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL502716 195235 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
117629482 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1588 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1594 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
2835 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
938 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
CHEMBL573 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
DB00627 9599 140 None - 2 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
135899171 22942 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 22942 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
122181102 128588 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2cccc(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589784 128588 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2cccc(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
46890302 14024 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1085842 14024 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
46890198 14089 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1086108 14089 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
46890578 13163 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1082294 13163 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
135899171 22942 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 22942 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
52941721 61739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1204125 61739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1615577 61739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
12002717 203521 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
CHEMBL565163 203521 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
52941721 61739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1204125 61739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1615577 61739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
54587625 68170 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770171 68170 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
117629482 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1588 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1594 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
2835 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
938 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
CHEMBL573 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
DB00627 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
11852982 21747 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208922 21747 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
11159621 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
5784 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
CHEMBL456145 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
DB05939 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
11159621 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
5784 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
CHEMBL456145 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
DB05939 9326 46 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
135899199 22999 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
CHEMBL1224293 22999 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
136088957 68177 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770178 68177 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
24811550 13452 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083450 13452 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
11624691 13999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1085711 13999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
137640776 163783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073322 163783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
117629482 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1588 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1594 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
2835 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
938 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
CHEMBL573 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
DB00627 9599 140 None -3 2 Human 6.8 pIC50 = 6.8 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
44445341 161027 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL398625 161027 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
156022048 184980 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649587 184980 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12002619 190959 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483141 190959 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
12003695 21751 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
CHEMBL1208926 21751 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
44591603 198481 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519689 198481 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
135502978 198768 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520136 198768 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
25101223 7935 7 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
5795 7935 7 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
CHEMBL490599 7935 7 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
49862073 21745 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208920 21745 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
12002520 190932 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL482943 190932 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
135899152 22998 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1224292 22998 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
11646179 191592 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL485185 191592 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890328 13453 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083451 13453 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
156021045 184910 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4648435 184910 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
156017210 184509 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
CHEMBL4642367 184509 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
11625092 13456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1083473 13456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
46890539 13812 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084841 13812 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
136375455 184333 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4640349 184333 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
12002523 178728 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL447050 178728 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003601 21752 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208987 21752 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
135899263 22884 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 307 7 1 3 3.7 O=c1[nH]c(CCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223875 22884 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 307 7 1 3 3.7 O=c1[nH]c(CCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156021045 184910 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4648435 184910 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
24741312 96174 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237036 96174 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
136088961 68224 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770357 68224 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
12003490 21748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208923 21748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
12003791 201608 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 201608 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 201608 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
11852982 21747 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208922 21747 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
16048997 101432 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 394 3 2 4 3.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2c(Cl)cncc2Cl)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252507 101432 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 394 3 2 4 3.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2c(Cl)cncc2Cl)CC1 10.1016/j.bmcl.2007.10.055
122181105 128595 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)ccc1O 10.1016/j.bmc.2015.02.018
CHEMBL3589791 128595 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)ccc1O 10.1016/j.bmc.2015.02.018
11493732 199879 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL522649 199879 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
54584718 68225 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770359 68225 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
122181142 128608 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3589836 128608 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11736428 195842 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 195842 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
16048992 101457 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252707 101457 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
135922719 191066 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
CHEMBL483996 191066 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
12003695 21751 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
CHEMBL1208926 21751 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
46890239 13706 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084448 13706 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
12003788 201720 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 201720 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 201720 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
136375410 184096 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4636989 184096 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
135899322 22964 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224146 22964 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048923 101431 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252506 101431 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
137661033 166266 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4101720 166266 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
122181140 128606 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589834 128606 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
15986930 191689 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485327 191689 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
156019027 184576 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
CHEMBL4643451 184576 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
135899198 22363 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1221438 22363 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899170 22944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224072 22944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
24741307 95510 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL236163 95510 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
24741307 95510 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
CHEMBL236163 95510 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
11660694 184847 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647392 184847 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
11493732 199879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL522649 199879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
12003596 21749 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208924 21749 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
12002619 190959 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483141 190959 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
117629482 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1588 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1594 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
2835 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
938 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
CHEMBL573 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
DB00627 9599 140 None -3 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
46890197 14031 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1085875 14031 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
137633734 163100 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4065654 163100 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
49862072 21744 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208919 21744 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
12003596 21749 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208924 21749 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
135899131 22907 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223959 22907 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048998 101407 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252307 101407 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
11299550 198786 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
CHEMBL520159 198786 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
44591602 195163 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL501585 195163 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
15986936 13873 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085150 13873 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
15986929 13931 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1085402 13931 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
135800176 96175 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237037 96175 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890164 14194 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086568 14194 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
11424509 195067 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL500239 195067 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
156021546 184965 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649305 184965 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12003785 203158 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL562632 203158 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
12002520 190932 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL482943 190932 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
135899325 22965 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 22965 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
17751630 13517 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083743 13517 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
137635425 162701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4060899 162701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890579 13788 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084798 13788 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
137662135 166129 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4100231 166129 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137645601 164630 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083723 164630 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11559598 128589 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2cccc(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589785 128589 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2cccc(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
11660694 184847 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647392 184847 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
11617151 95414 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL235741 95414 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
16048919 101458 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
CHEMBL252708 101458 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
12002522 195235 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL502716 195235 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
137653428 165322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091542 165322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
42625474 190957 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483139 190957 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
42625379 198870 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520299 198870 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890327 13372 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083138 13372 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
135416388 14296 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1087302 14296 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
12003490 21748 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208923 21748 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
42625213 199082 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520620 199082 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890163 14193 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086567 14193 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
12003879 199121 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL520675 199121 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
156020475 184853 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
CHEMBL4647545 184853 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
12002523 178728 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL447050 178728 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
46890165 14086 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086103 14086 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
46890501 14018 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085816 14018 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
137647495 164635 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083762 164635 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11508815 128585 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccc(F)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589779 128585 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccc(F)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
122181104 128593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 413 6 2 2 5.6 O=C(CCc1ccc(-c2ccccc2C(F)(F)F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589789 128593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 413 6 2 2 5.6 O=C(CCc1ccc(-c2ccccc2C(F)(F)F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
90645405 119310 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3299113 119310 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
136127016 22943 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224071 22943 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135800175 95511 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nnc(-c2ccc(O)cc2)o1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL236164 95511 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nnc(-c2ccc(O)cc2)o1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44579763 193762 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490600 193762 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
137652577 165539 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093990 165539 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11560300 95314 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL235256 95314 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
24811547 14148 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086355 14148 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
11638560 193822 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491002 193822 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
42625382 191591 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
CHEMBL485184 191591 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
11736428 195842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 195842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003880 195513 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL504980 195513 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
44580007 193726 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
CHEMBL490215 193726 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
12003601 21752 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208987 21752 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
135399731 190936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
CHEMBL482963 190936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
46890500 14017 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085815 14017 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
24741306 173735 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL428724 173735 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890401 14059 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086031 14059 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
42625380 191190 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 407 5 3 8 1.6 Cn1c(=O)c2c(CCC(=O)Nc3ccccc3C(=O)O)nnn2c2ccc(O)cc21 10.1021/jm900151e
CHEMBL484605 191190 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 407 5 3 8 1.6 Cn1c(=O)c2c(CCC(=O)Nc3ccccc3C(=O)O)nnn2c2ccc(O)cc21 10.1021/jm900151e
44591586 190940 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL482979 190940 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
137648318 164411 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4081260 164411 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
122181106 128596 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)c(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589792 128596 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)c(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
137632012 163435 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4069406 163435 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003791 201608 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 201608 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 201608 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
136127015 22904 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 4 1 4 2.4 O=c1[nH]c(OC/C=C/c2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223956 22904 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 4 1 4 2.4 O=c1[nH]c(OC/C=C/c2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899149 22909 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223960 22909 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135922723 190941 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 364 5 3 5 3.2 O=C(CCc1noc2c1Cc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL482980 190941 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 364 5 3 5 3.2 O=C(CCc1noc2c1Cc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
49862072 21744 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208919 21744 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
137654580 165801 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4096635 165801 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003694 7927 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
5793 7927 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
CHEMBL1208986 7927 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
156017987 184698 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 358 5 3 4 3.4 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nn1cccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4645273 184698 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 358 5 3 4 3.4 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nn1cccc1C(=O)O 10.1016/j.bmcl.2020.127105
11560300 95314 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL235256 95314 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
11560300 95314 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235256 95314 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135800194 96266 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237248 96266 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135466520 190996 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483353 190996 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
135416384 191603 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL485196 191603 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
136086823 13741 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1084576 13741 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
135416388 14296 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1087302 14296 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
136088958 68220 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770353 68220 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
12002618 198770 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 198770 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 198770 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 198770 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
137650474 164058 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4076822 164058 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003788 201720 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 201720 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 201720 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
136127010 22858 11 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 22858 11 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156020831 184849 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647398 184849 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12003692 21753 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208988 21753 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
44591604 191602 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL485195 191602 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
136088962 68175 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770176 68175 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
156016157 184557 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
CHEMBL4643073 184557 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
12003880 195513 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL504980 195513 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
136127017 22985 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
CHEMBL1224222 22985 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
136000579 68174 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770175 68174 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
46890271 14149 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 355 5 4 4 2.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(O)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086356 14149 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 355 5 4 4 2.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(O)CC1 10.1016/j.bmcl.2010.04.001
12002521 191600 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL485194 191600 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
46890268 13378 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1083174 13378 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
12003879 199121 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL520675 199121 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
135899109 22986 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224223 22986 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
135899153 22984 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1224221 22984 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
135899247 22860 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 5 1 3 2.9 O=c1[nH]c(CCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223823 22860 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 5 1 3 2.9 O=c1[nH]c(CCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899110 23000 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224294 23000 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
12003694 7927 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
5793 7927 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
CHEMBL1208986 7927 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
135812996 22945 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccccc1OCCCOc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1224073 22945 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccccc1OCCCOc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
46890238 13872 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085149 13872 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
12003790 202834 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL560406 202834 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
135800177 152729 7 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 152729 7 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
156016715 184454 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
CHEMBL4641756 184454 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
11183317 198249 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL519338 198249 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
135899130 22947 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224075 22947 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
44591586 190940 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL482979 190940 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
136127012 22885 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 321 8 1 3 4.1 O=c1[nH]c(CCCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223876 22885 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 321 8 1 3 4.1 O=c1[nH]c(CCCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890240 13875 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085156 13875 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
46890301 13971 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085616 13971 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
11516324 190995 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483352 190995 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
15986931 199015 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL520513 199015 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
136088960 68222 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1770355 68222 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
135899178 22982 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 22982 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
12002802 202612 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
CHEMBL558334 202612 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
117629482 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1588 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1594 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
2835 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
938 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
CHEMBL573 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
DB00627 9599 140 None -3 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
44591604 191602 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL485195 191602 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
11610363 96265 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237247 96265 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
156010038 183809 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4632359 183809 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
24811199 13373 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083139 13373 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
12002524 198561 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
CHEMBL519811 198561 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
44591602 195163 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL501585 195163 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003692 21753 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208988 21753 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
44579742 193823 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491003 193823 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
16048770 101406 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252306 101406 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
156013148 184247 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4639053 184247 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
11523335 128591 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1ccccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
CHEMBL3589787 128591 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1ccccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
137661636 166042 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099238 166042 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890537 13810 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084839 13810 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
16048921 161796 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401470 161796 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
122181141 128607 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 377 6 4 4 4.0 O=C(CCc1ccc(-c2ccc(O)cc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589835 128607 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 377 6 4 4 4.0 O=C(CCc1ccc(-c2ccc(O)cc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
24741310 96397 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL237543 96397 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
24741310 96397 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237543 96397 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
137637662 163020 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4064786 163020 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
135899244 22883 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 293 6 1 3 3.3 O=c1[nH]c(CCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223874 22883 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 293 6 1 3 3.3 O=c1[nH]c(CCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890300 14187 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1086541 14187 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
42625218 190958 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483140 190958 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
46890580 13789 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1084799 13789 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
46890270 14147 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086354 14147 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
135800194 96266 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL237248 96266 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11736428 195842 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 195842 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003791 201608 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 201608 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 201608 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
135899154 22981 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224218 22981 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
12002524 198561 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
CHEMBL519811 198561 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
136375437 184860 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647670 184860 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
135899325 22965 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 22965 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899324 22963 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 327 7 1 6 2.2 COc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224145 22963 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 327 7 1 6 2.2 COc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
135899178 22982 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 22982 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156010038 183809 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4632359 183809 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
16048768 101225 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
CHEMBL251222 101225 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
137659759 166046 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099278 166046 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003787 202621 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL558463 202621 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
137639493 163690 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4072283 163690 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
135899321 22887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 281 5 1 4 2.1 O=c1[nH]c(COCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223878 22887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 281 5 1 4 2.1 O=c1[nH]c(COCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048843 161170 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
CHEMBL398762 161170 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
11424509 195067 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL500239 195067 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
46890237 13871 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085148 13871 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
135966934 13614 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084030 13614 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
46890298 13934 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085414 13934 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
12002518 195658 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL507182 195658 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002518 195658 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL507182 195658 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 198770 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 198770 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 198770 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
CHEMBL520137 198770 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
156020512 184883 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647933 184883 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
11624691 13999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL1085711 13999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
137641317 163790 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073374 163790 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137648386 164551 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4082765 164551 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12002616 190960 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483142 190960 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
16048995 101430 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252505 101430 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
11646494 128587 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 7 2 3 4.6 COc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
CHEMBL3589783 128587 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 7 2 3 4.6 COc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
11516424 14087 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1086104 14087 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
12002521 191600 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL485194 191600 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
135401975 101523 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL253128 101523 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
11647028 95457 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235954 95457 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11501698 199349 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL521326 199349 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
136086829 14110 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
CHEMBL1086225 14110 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
46890269 14146 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086353 14146 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
15986755 190897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL482698 190897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
46890299 13987 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085655 13987 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
11736428 195842 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 195842 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12002618 198770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 198770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 198770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
CHEMBL520137 198770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
12002517 198661 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519966 198661 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12003597 21750 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208925 21750 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
11710202 128586 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
CHEMBL3589782 128586 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
16048840 100819 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL248851 100819 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
44591601 191090 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL484172 191090 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
122181103 128592 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccccc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589788 128592 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccccc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
135899300 22886 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 6 1 4 2.7 O=c1[nH]c(OCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223877 22886 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 6 1 4 2.7 O=c1[nH]c(OCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890538 13811 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084840 13811 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
12003791 201608 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 201608 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 201608 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
12002616 190960 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483142 190960 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
11581300 128594 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccccc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589790 128594 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccccc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
135899150 22946 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1cccc(OCCCOc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
CHEMBL1224074 22946 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1cccc(OCCCOc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
11501164 193957 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 349 6 2 3 4.1 COc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL492220 193957 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 349 6 2 3 4.1 COc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
135401974 161502 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL399859 161502 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
44591601 191090 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL484172 191090 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
137653026 165486 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093294 165486 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890275 13302 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082823 13302 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
11617480 95456 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235952 95456 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890577 13444 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083442 13444 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
136086824 13615 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084031 13615 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
12003788 201720 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 201720 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 201720 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
12003597 21750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208925 21750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
12002525 199122 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
CHEMBL520676 199122 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
11299550 198786 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
CHEMBL520159 198786 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
122181107 128597 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)c(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589793 128597 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)c(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
46890199 13930 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085401 13930 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
135899280 22906 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 308 5 2 4 1.6 O=C(CCc1ccccc1)NCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1223958 22906 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 308 5 2 4 1.6 O=C(CCc1ccccc1)NCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
11625092 13456 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL1083473 13456 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
11617151 95414 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235741 95414 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11631886 128590 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2cccc(O)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589786 128590 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2cccc(O)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
136375465 183912 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4633857 183912 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
49862073 21745 1 None - 0 Mouse 6.0 pIC50 = 6 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208920 21745 1 None - 0 Mouse 6.0 pIC50 = 6 Binding
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
135887290 13759 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1084657 13759 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
6436431 68475 4 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 4 1 3 0.6 CCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771638 68475 4 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 4 1 3 0.6 CCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
54580649 68521 2 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 5 1 3 1.4 O=C(O)/C=C/C(=O)OCCc1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL1771739 68521 2 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 5 1 3 1.4 O=C(O)/C=C/C(=O)OCCc1ccccc1 10.1016/j.bmcl.2010.11.091
117629482 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1588 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1594 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
2835 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
938 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
CHEMBL573 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
DB00627 9599 140 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
135887288 14388 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
CHEMBL1088074 14388 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
135887285 14210 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
CHEMBL1086658 14210 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
135416391 13692 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084393 13692 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
135800194 96266 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
CHEMBL237248 96266 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
11041813 100526 22 None - 1 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1021/jm030888c
CHEMBL247317 100526 22 None - 1 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1021/jm030888c
135887289 13693 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084394 13693 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
5787 9779 119 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
637542 9779 119 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
CHEMBL66879 9779 119 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
DB04066 9779 119 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
643403 108369 79 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccoc1 10.1016/j.bmcl.2010.11.091
CHEMBL298683 108369 79 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccoc1 10.1016/j.bmcl.2010.11.091
676464 96651 75 None - 1 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1021/jm030888c
CHEMBL237788 96651 75 None - 1 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1021/jm030888c
135416388 14296 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1087302 14296 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
776416 25710 108 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800896z
CHEMBL128604 25710 108 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800896z
776416 25710 108 None -1 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm030888c
CHEMBL128604 25710 108 None -1 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm030888c
11830866 26181 35 None - 1 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 4 2 2 1.9 O=C(O)c1cc(CCc2ccccc2)[nH]n1 10.1021/jm030888c
CHEMBL129385 26181 35 None - 1 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 4 2 2 1.9 O=C(O)c1cc(CCc2ccccc2)[nH]n1 10.1021/jm030888c
5369209 9369 81 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
5786 9369 81 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL589586 9369 81 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
DB14219 9369 81 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
10878560 25919 3 None - 1 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 3 2 2 2.0 Cc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
CHEMBL128949 25919 3 None - 1 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 3 2 2 2.0 Cc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
13169286 25612 1 None - 1 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 266 11 2 2 4.2 CCCCCCCCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm030888c
CHEMBL128077 25612 1 None - 1 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 266 11 2 2 4.2 CCCCCCCCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm030888c
135416393 14401 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1088213 14401 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
135416392 14209 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 14209 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
135416392 14209 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 14209 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
54582649 68524 1 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 224 4 1 3 1.5 O=C(O)/C=C/C(=O)OCc1cccc(F)c1 10.1016/j.bmcl.2010.11.091
CHEMBL1771745 68524 1 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 224 4 1 3 1.5 O=C(O)/C=C/C(=O)OCc1cccc(F)c1 10.1016/j.bmcl.2010.11.091
135887289 13693 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084394 13693 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
5816396 68479 6 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 200 7 1 3 1.8 CCCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771642 68479 6 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 200 7 1 3 1.8 CCCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
135416391 13692 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084393 13692 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
135416388 14296 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1087302 14296 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
117629482 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
1588 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
1594 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
2835 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
938 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
CHEMBL573 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
DB00627 9599 140 None 3 2 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
648852 123688 91 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm800896z
CHEMBL338405 123688 91 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm800896z
6437229 68519 9 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 206 4 1 3 1.4 O=C(O)/C=C/C(=O)OCc1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL1771737 68519 9 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 206 4 1 3 1.4 O=C(O)/C=C/C(=O)OCc1ccccc1 10.1016/j.bmcl.2010.11.091
648852 123688 91 None -1 2 Rat 5.5 pKi = 5.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm030888c
CHEMBL338405 123688 91 None -1 2 Rat 5.5 pKi = 5.5 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm030888c
135887288 14388 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
CHEMBL1088074 14388 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
10857469 125335 4 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2ccc(Cl)cc2)[nH]n1 10.1021/jm030888c
CHEMBL341520 125335 4 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2ccc(Cl)cc2)[nH]n1 10.1021/jm030888c
818267 125230 83 None - 1 Rat 4.4 pKi = 4.4 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 2 2 2 2.1 Cc1ccc(-c2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
CHEMBL341154 125230 83 None - 1 Rat 4.4 pKi = 4.4 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 2 2 2 2.1 Cc1ccc(-c2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
135416394 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
135416392 14209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 14209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
135800194 96266 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
CHEMBL237248 96266 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
5358902 68474 79 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 144 3 1 3 0.2 CCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771637 68474 79 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 144 3 1 3 0.2 CCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
6057891 68476 33 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 3 1 3 0.6 CC(C)OC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771639 68476 33 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 3 1 3 0.6 CC(C)OC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
3203 7726 111 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2010.11.091
444539 7726 111 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL27246 7726 111 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2010.11.091
117629482 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
1588 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
1594 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
2835 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
938 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
CHEMBL573 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
DB00627 9599 140 None -3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
11776293 156036 8 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1021/jm030888c
CHEMBL394441 156036 8 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1021/jm030888c
11159621 9326 46 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 9326 46 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 9326 46 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 9326 46 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
735981 68526 101 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 154 2 1 2 1.8 O=C(O)/C=C/c1cccs1 10.1016/j.bmcl.2010.11.091
CHEMBL1771765 68526 101 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 154 2 1 2 1.8 O=C(O)/C=C/c1cccs1 10.1016/j.bmcl.2010.11.091
14112183 68520 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 4 1 3 1.9 CC(OC(=O)/C=C/C(=O)O)c1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL1771738 68520 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 4 1 3 1.9 CC(OC(=O)/C=C/C(=O)O)c1ccccc1 10.1016/j.bmcl.2010.11.091
574310 25728 148 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1021/jm030888c
CHEMBL128679 25728 148 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1021/jm030888c
135416394 9338 52 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 9338 52 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 9338 52 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 9338 52 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
11746440 26175 1 None - 1 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 230 5 2 2 2.3 O=C(O)c1cc(CCCc2ccccc2)[nH]n1 10.1021/jm030888c
CHEMBL129326 26175 1 None - 1 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 230 5 2 2 2.3 O=C(O)c1cc(CCCc2ccccc2)[nH]n1 10.1021/jm030888c
4430637 123615 93 None - 1 Rat 4.2 pKi = 4.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 222 2 2 2 2.4 O=C(O)c1cc(-c2cccc(Cl)c2)[nH]n1 10.1021/jm030888c
CHEMBL338017 123615 93 None - 1 Rat 4.2 pKi = 4.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 222 2 2 2 2.4 O=C(O)c1cc(-c2cccc(Cl)c2)[nH]n1 10.1021/jm030888c
135416393 14401 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1088213 14401 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
10922388 25288 3 None - 1 Rat 4.2 pKi = 4.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 232 4 2 3 1.7 COc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
CHEMBL127387 25288 3 None - 1 Rat 4.2 pKi = 4.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 232 4 2 3 1.7 COc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
776421 96703 108 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1021/jm030888c
CHEMBL238002 96703 108 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1021/jm030888c
10103897 68478 3 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 186 6 1 3 1.4 CCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771641 68478 3 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 186 6 1 3 1.4 CCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
13153555 100638 27 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm800896z
CHEMBL247921 100638 27 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm800896z
1591 6919 63 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1021/jm030888c
6485181 6919 63 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1021/jm030888c
CHEMBL428730 6919 63 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1021/jm030888c
5475335 68477 28 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 172 5 1 3 1.0 CCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771640 68477 28 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 172 5 1 3 1.0 CCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
135416392 14209 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 14209 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
643402 68525 99 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccco1 10.1016/j.bmcl.2010.11.091
CHEMBL1771761 68525 99 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccco1 10.1016/j.bmcl.2010.11.091
117629482 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1588 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1594 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
2835 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
938 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
CHEMBL573 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
DB00627 9599 140 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
135887290 13759 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1084657 13759 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
54583606 68523 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 240 4 1 3 2.0 O=C(O)/C=C/C(=O)OCc1cccc(Cl)c1 10.1016/j.bmcl.2010.11.091
CHEMBL1771744 68523 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 240 4 1 3 2.0 O=C(O)/C=C/C(=O)OCc1cccc(Cl)c1 10.1016/j.bmcl.2010.11.091
135887285 14210 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
CHEMBL1086658 14210 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
54582648 68522 1 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 284 4 1 3 2.1 O=C(O)/C=C/C(=O)OCc1cccc(Br)c1 10.1016/j.bmcl.2010.11.091
CHEMBL1771743 68522 1 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 284 4 1 3 2.1 O=C(O)/C=C/C(=O)OCc1cccc(Br)c1 10.1016/j.bmcl.2010.11.091
117629482 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 9599 140 None - 2 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
117629482 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
117629482 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
117629482 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1588 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1588 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1588 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1594 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1594 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1594 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
2835 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
2835 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
2835 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
938 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
938 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
938 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
CHEMBL573 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
CHEMBL573 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
CHEMBL573 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
DB00627 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
DB00627 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
DB00627 9599 140 None -3 2 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
637568 224519 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
Drug Central 144 2 0 4 -0.1 COC(=O)\C=C\C(=O)OC None
117629482 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 9599 140 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
117629482 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 9599 140 None 3 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
5369209 9369 81 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
5786 9369 81 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
CHEMBL589586 9369 81 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
DB14219 9369 81 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
135416394 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
5788 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
73755154 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
CHEMBL1086657 9338 52 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
1591 6919 63 None - 1 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 12930155
6485181 6919 63 None - 1 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 12930155
CHEMBL428730 6919 63 None - 1 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 12930155