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 75259 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 75259 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 7374 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 7374 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 75257 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 75257 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 75262 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 75262 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 162287 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 162287 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 162287 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 162287 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 177030 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 177030 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 93709 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 93709 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 6745 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 6745 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 177675 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 177675 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 88638 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 88638 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 184187 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 184187 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 88638 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 88638 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 93709 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 93709 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 61399 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 61399 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 69917 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 69917 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 69920 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 69920 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 69939 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 69939 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 162512 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 162512 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 112533 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 112533 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 162512 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 162512 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 76040 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 76040 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 18938 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 18938 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 95188 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 95188 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 69928 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 69928 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 58038 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 58038 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 58041 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 58041 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 2548 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 2548 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 2548 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 2548 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 89928 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 89928 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 93863 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 93863 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 6600 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 6600 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 75247 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 75247 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 126 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 126 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 126 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 126 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 126 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 126 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 184909 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 184909 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 75246 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 75246 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 158760 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 158760 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 83454 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 83454 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 194941 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 194941 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 194941 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 195842 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 195842 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 154014 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 154014 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 154723 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 154723 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 6724 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 6724 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 58061 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 58061 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 76351 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 76351 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 69926 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 69926 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 76115 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 76115 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 75235 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 75235 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 76117 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 76117 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 145951 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 145951 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 184535 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 184535 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 1152 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 1152 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 1152 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 145951 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 145951 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 195500 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 195500 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 138156 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 138156 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 169652 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 169652 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 165495 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 165495 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 141606 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 141606 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 93791 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 93791 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 149578 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 149578 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 149283 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 149283 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 69916 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 69916 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 85607 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 85607 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 85607 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 85607 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 112483 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 112483 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 58048 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 58048 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 58056 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 58056 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 76473 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 76473 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 7107 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 7107 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 75258 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 75258 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 7215 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 7215 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 58046 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 58046 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 156321 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 156321 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 157011 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 157011 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 89622 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 89622 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 186949 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 186949 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 187091 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 187091 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
13557 1106 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 CC1=NOC(=C1)C(=O)O 10.1016/j.bmcl.2007.06.028
853085 1106 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 CC1=NOC(=C1)C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL393428 1106 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 CC1=NOC(=C1)C(=O)O 10.1016/j.bmcl.2007.06.028
12003788 194941 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 194941 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 194941 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 196742 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 196742 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 75240 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 75240 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 165815 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 165815 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 94655 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 94655 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 94682 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 94682 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 69929 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 69929 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 93757 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 93757 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 69949 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 69949 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 7287 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 7287 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 69921 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 69921 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 69871 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 69871 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 76112 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 76112 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 16210 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 16210 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 177778 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 177778 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 187160 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 187160 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 112481 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 112481 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 131 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 131 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 131 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 178070 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 178070 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 58032 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 58032 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 76107 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 76107 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 6831 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 6831 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 178068 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 178068 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 58034 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 58034 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 177797 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 177797 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 178104 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 178104 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 147734 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 147734 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 61404 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 61404 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 88534 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 88534 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 88537 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 88537 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 7180 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 7180 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 2560 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 2560 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 2560 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 2560 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 75040 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 75040 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 75263 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 75263 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 76113 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 76113 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 156149 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 156149 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 136766 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 136766 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 177317 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 177317 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 94631 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 94631 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 75237 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 75237 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 145951 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 145951 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 16193 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 16193 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 144 131 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 144 131 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 144 131 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 93355 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 93355 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 76348 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 76348 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 2548 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 2548 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 2548 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 2548 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 162287 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 162287 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 162287 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 162287 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 147518 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 147518 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 6969 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 6969 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 75235 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 75235 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 184157 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 184157 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 75239 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 75239 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 16086 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 16086 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 154391 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 154391 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 69951 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 69951 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 69945 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 69945 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 76347 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 76347 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 69947 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 69947 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 186965 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 186965 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 93863 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 93863 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 89876 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 89876 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 88536 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 88536 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 6725 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 6725 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 147524 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 147524 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 184824 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 184824 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 75244 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 75244 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 69919 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 69919 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 16170 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 16170 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 159263 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 159263 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 159350 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 159350 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 186895 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 186895 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 184118 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 184118 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 137618 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 137618 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 76111 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 76111 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 157851 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 157851 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 76476 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 76476 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 3559 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 3559 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 3559 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 3559 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 75256 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 75256 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 75260 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 75260 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 84271 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 84271 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 84271 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 84271 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 84907 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 84907 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 177133 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 177133 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 6833 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 6833 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 152223 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 152223 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 69922 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 69922 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 7524 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 7524 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 7524 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 7524 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 1001 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 1001 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 1001 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 165782 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 165782 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 166956 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 166956 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 187158 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 187158 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 147563 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 147563 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 165443 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 165443 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 76116 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 76116 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 1027 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 1027 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 1027 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 7437 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 7437 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 69952 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 69952 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 7040 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 7040 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 76118 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 76118 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 75236 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 75236 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 150178 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 150178 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 155017 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 155017 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 93355 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 93355 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 76349 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 76349 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 76475 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 76475 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 7038 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 7038 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 75249 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 75249 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 157856 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 157856 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 186966 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 186966 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 187101 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 187101 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 194829 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 194829 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 194829 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 136550 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 136550 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 148783 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 148783 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 7184 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 7184 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 162960 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 162960 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 162960 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 162960 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 6654 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 6654 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 69932 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 69932 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 184179 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 184179 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 7524 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 7524 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 145638 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 145638 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 143 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 143 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 143 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 89399 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 89399 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 2560 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 2560 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 2560 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 2560 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 84772 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 84772 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 1122 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 1122 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 1122 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 7064 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 7064 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 58055 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 58055 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 7185 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 7185 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 76108 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 76108 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 7437 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 7437 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 7039 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 7039 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 156656 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 156656 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 137619 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 137619 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 16193 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 16193 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 93667 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 93667 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 147562 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 147562 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 196055 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 196055 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 147517 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 147517 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 69948 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 69948 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 75242 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 75242 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 69925 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 69925 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 156241 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 156241 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 84906 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 84906 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 184812 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 184812 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 177449 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 177449 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 112415 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 112415 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 7286 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 7286 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 147255 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 147255 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 89491 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 89491 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 89491 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 89491 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 6842 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 6842 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 89491 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 89491 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 2552 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 2552 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 2552 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 184813 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 184813 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 69931 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 69931 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 158707 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 158707 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 116846 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 116846 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 1058 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 1058 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 1058 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 58051 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 58051 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 112519 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 112519 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 58058 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 58058 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 162222 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 162222 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 7183 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 7183 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 76119 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 76119 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 162222 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 162222 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 76474 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 76474 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 7162 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 7162 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 75245 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 75245 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 69952 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 69952 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 84892 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 84892 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 177352 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 177352 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 167382 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 167382 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 196054 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 196054 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 58040 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 58040 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 69918 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 69918 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 6832 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 6832 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 83459 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 83459 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 6920 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 6920 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 7629 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 7629 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 69930 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 69930 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 61400 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 61400 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 75233 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 75233 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 177730 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 177730 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 93750 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 93750 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 69934 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 69934 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 161911 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 161911 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 61402 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 61402 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 158538 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 158538 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 75256 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 75256 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 57843 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 57843 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 7375 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 7375 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 162960 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 162960 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 162960 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 162960 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 186983 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 186983 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 58057 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 58057 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 7214 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 7214 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 75232 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 75232 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 75253 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 75253 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 58033 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 58033 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 76114 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 76114 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 58039 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 58039 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 69946 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 69946 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 69924 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 69924 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 178081 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 178081 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 186947 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 186947 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 61396 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 61396 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 58036 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 58036 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 94683 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 94683 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 84748 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 84748 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 58050 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 58050 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 159267 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 159267 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 58062 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 58062 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 184216 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 184216 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 69944 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 69944 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 193100 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 193100 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 16210 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 16210 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 145949 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 145949 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 61403 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 61403 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 152411 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 152411 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 89810 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 89810 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 58049 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 58049 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 61446 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 61446 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 156911 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 156911 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 112533 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 112533 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 112421 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 112421 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 76113 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 76113 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 143 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 143 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 143 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 149833 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 149833 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 7238 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 7238 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 58045 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 58045 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 63818 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 63818 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 193100 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 193100 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 195833 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 195833 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 61448 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 61448 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 75261 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 75261 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 159022 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 159022 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 89876 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 89876 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 75254 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 75254 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 75260 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 75260 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 57843 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 57843 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 75259 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 75259 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 75254 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 75254 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 192570 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 192570 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 1965 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 1965 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 1965 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 2548 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 2548 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 2548 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 2548 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 88535 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 88535 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 89929 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 89929 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 6601 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 6601 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 61451 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 61451 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 157279 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 157279 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 112422 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 112422 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 112518 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 112518 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 84749 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 84749 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 58059 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 58059 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 69923 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 69923 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 7338 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 7338 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 83462 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 83462 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 69955 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 69955 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 69941 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 69941 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 184209 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 184209 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 76118 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 76118 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 84757 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 84757 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 89400 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 89400 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 6606 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 6606 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 88490 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 88490 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 94450 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 94450 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 196379 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 196379 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 58054 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 58054 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 7130 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 7130 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 88539 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 88539 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 6672 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 6672 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 157004 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 157004 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 112480 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 112480 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 194829 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 194829 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 194829 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 58042 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 58042 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 162017 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 162017 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 162017 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 162017 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 6391 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 6391 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 193021 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 193021 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 145638 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 145638 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 7246 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 7246 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 94044 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 94044 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 2560 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 2560 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 2560 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 2560 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 136564 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 136564 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 84271 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 84271 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 75243 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 75243 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 1022 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 1022 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 1022 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 58060 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 58060 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 75248 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 75248 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 58060 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 58060 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 58044 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 58044 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 126 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 126 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 126 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 184210 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 184210 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 84876 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 84876 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 7285 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 7285 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 177468 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 177468 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 58034 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 58034 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 7245 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 7245 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 150121 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 150121 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 75255 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 75255 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 75256 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 75256 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 75259 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 75259 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 184217 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 184217 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 16170 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 16170 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 18938 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 18938 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 88638 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 88638 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 93716 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 93716 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 61447 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 61447 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 83463 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 83463 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 155016 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 155016 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 6723 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 6723 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 7181 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 7181 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 192091 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 192091 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 112423 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 112423 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 259 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 259 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 259 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 69943 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 69943 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 260 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 260 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
76 260 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 260 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 260 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 153285 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 153285 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 7213 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 7213 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 76472 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 76472 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 187043 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 187043 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 85011 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 85011 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 137620 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 137620 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 7182 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 7182 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 76350 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 76350 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 54965 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 54965 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 54965 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 93833 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 93833 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 93864 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 93864 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 157632 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 157632 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 152208 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 152208 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 83459 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 83459 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 84946 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 84946 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 76114 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 76114 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 94748 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 94748 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 112534 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 112534 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 69938 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 69938 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 89190 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 89190 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 57843 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 57843 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 88639 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 88639 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 88639 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 88639 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 94632 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 94632 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 58047 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 58047 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 88734 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 88734 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 7193 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 7193 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 88734 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 88734 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 3559 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 3559 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 3559 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 3559 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 58034 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 58034 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 184178 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 184178 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 7227 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 7227 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 16086 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 16086 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 85607 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 85607 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 85607 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 85607 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 186948 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 186948 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 58052 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 58052 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 137602 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 137602 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 93621 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 93621 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 75241 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 75241 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 184910 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 184910 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 149257 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 149257 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 69937 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 69937 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 158543 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 158543 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 154248 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 154248 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 112532 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 112532 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 202636 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 202636 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 1058 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 1058 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 1058 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 6680 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 6680 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 178131 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 178131 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 6921 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 6921 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 61398 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 61398 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 58053 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 58053 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 84271 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 84271 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 69950 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 69950 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 93790 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 93790 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 69954 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 69954 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 112535 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 112535 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 192303 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 192303 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 75265 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 75265 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 76106 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 76106 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 121830 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 121830 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 187159 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 187159 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 136357 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 136357 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 159487 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 159487 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 137967 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 137967 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 178074 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 178074 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 61450 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 61450 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 69933 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 69933 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 7616 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 7616 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 184287 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 184287 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 69935 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 69935 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 191989 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 191989 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 84666 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 84666 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 7016 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 7016 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 7017 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 7017 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 152409 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 152409 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 192236 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 192236 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 184118 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 184118 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 178186 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 178186 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 150180 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 150180 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 88682 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 88682 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 18956 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 18956 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 147522 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 147522 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 168977 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 168977 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 58037 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 58037 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 88489 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 88489 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 149322 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 149322 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 167175 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 167175 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 3559 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 3559 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 3559 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 3559 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 75235 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 75235 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 155922 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 155922 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 149322 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 149322 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 76471 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 76471 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 178201 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 178201 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 58043 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 58043 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 76109 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 76109 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 69954 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 69954 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 149578 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 149578 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 184490 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 184490 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 89928 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 89928 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 149578 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 149578 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 184191 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 184191 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 76106 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 76106 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 61449 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 61449 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 131 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 131 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 131 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 76110 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 76110 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 88681 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 88681 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 18938 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 18938 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 69927 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 69927 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 18938 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 18938 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 93418 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 93418 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 93832 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 93832 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 61401 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 61401 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 93751 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 93751 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 157772 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 157772 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 69953 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 69953 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 112482 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 112482 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 94656 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 94656 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 94346 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 94346 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 69940 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 69940 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 1131 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 1131 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 1131 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 7376 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 7376 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 88735 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 88735 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 69936 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 69936 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 89490 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 89490 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 187068 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 187068 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 61397 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 61397 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 75238 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 75238 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 196598 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 196598 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 6681 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 6681 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 187044 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 187044 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 177554 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 177554 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 69942 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 69942 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 145671 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 145671 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 6843 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 6843 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 75234 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 75234 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
13557 1106 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 CC1=NOC(=C1)C(=O)O 10.1074/jbc.m701866200
853085 1106 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 CC1=NOC(=C1)C(=O)O 10.1074/jbc.m701866200
CHEMBL393428 1106 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 CC1=NOC(=C1)C(=O)O 10.1074/jbc.m701866200
11550911 95188 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 95188 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 167382 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 167382 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 89928 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 89928 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 149257 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 149257 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 259 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 259 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 259 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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
108 111 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
1590 111 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
3505 111 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
CHEMBL1741437 111 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
1596 260 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 260 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
76 260 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 260 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 260 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
13558 1041 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 242 3 2 4 0.9 C(CCC)N1C(NC(C=2NC(=NC12)Cl)=O)=O None
59299562 1041 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 242 3 2 4 0.9 C(CCC)N1C(NC(C=2NC(=NC12)Cl)=O)=O None
CHEMBL3732182 1041 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 242 3 2 4 0.9 C(CCC)N1C(NC(C=2NC(=NC12)Cl)=O)=O None
13559 1135 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 460 9 1 9 2.1 C(CCC)N1C(N(C(C=2NC(=NC12)Cl)=O)CCCN3N=C(N=N3)CC4=CC=C(C=C4)F)=O None
59395852 1135 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 460 9 1 9 2.1 C(CCC)N1C(N(C(C=2NC(=NC12)Cl)=O)CCCN3N=C(N=N3)CC4=CC=C(C=C4)F)=O None
1059 750 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
264 750 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 750 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 750 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 609 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 609 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 609 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 3005 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 3005 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 3005 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 3005 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 939 111 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 939 111 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 939 111 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 2591 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 2591 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 2591 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 2591 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 260 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 260 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 260 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 260 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
76 260 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
76 260 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 260 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 260 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 260 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 260 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 1096 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 1096 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 2548 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 2548 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 2548 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 2548 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 1152 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 1152 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 1152 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 1001 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 1001 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 1001 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
13359 1099 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 442 9 3 7 4.8 CNCCNCC1=CC=CC(=C1)C2=NC(C3=C(C)ON=C3C)=C(C)C(NC4=CC=CC=C4)=N2 None
146188223 1099 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 442 9 3 7 4.8 CNCCNCC1=CC=CC(=C1)C2=NC(C3=C(C)ON=C3C)=C(C)C(NC4=CC=CC=C4)=N2 None
46215799 1880 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 1880 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 1880 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 2552 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 2552 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 2552 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 2560 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 2560 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 2560 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 2560 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 3559 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 3559 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 3559 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 3559 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 609 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 609 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 609 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 144 131 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 144 131 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 144 131 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
108 111 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 111 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 111 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 111 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 259 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 126 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 126 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 126 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 126 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 126 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 126 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 188625 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 188625 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
13557 1106 111 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.
Guide to Pharmacology 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 17452318
853085 1106 111 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.
Guide to Pharmacology 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 17452318
CHEMBL393428 1106 111 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.
Guide to Pharmacology 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 17452318
12003694 1144 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 1144 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 1144 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 1022 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 1022 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 1022 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 1058 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 1058 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 1058 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 1027 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 1027 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 1027 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 260 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 260 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
76 260 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 260 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 260 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 7315 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 7315 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 6684 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 6684 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 177648 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 177648 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 177661 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 177661 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 6530 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 6530 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 89622 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 89622 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 178215 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 178215 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 259 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 259 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 259 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 177924 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 177924 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 177974 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 177974 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 6906 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 6906 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 6849 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 6849 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 177398 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 177398 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 7101 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 7101 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 1066 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 1066 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 1066 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 6531 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 6531 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 7103 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 7103 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 7099 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 7099 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 7158 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 7158 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 177655 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 177655 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 7314 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 7314 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 7159 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 7159 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 177698 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 177698 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 6847 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 6847 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 7422 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 7422 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 88539 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 88539 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 58060 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 58060 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 75235 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 75235 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 193620 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 193872 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 193921 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 194116 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 194273 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 6934 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 6934 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 178167 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 178167 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 7199 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 7199 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 177310 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 177310 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 7415 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 7415 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 7317 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 7317 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 7100 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 7100 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 145638 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 145638 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 177192 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 177192 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 88735 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 88735 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 7259 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 7259 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 7252 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 7252 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 7421 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 7421 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 88734 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 88734 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 184209 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 184209 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 184210 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 184210 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 61445 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 61445 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 88734 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 88734 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 6847 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 6847 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 145951 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 145951 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 145951 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 145951 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 61397 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 61397 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 61447 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 61447 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 186948 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 186948 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 177505 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 177505 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 121831 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 121831 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 121830 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 121830 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 61402 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 61402 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 184535 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 184535 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 7214 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 7214 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 61449 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 61449 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 94346 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 94346 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 177352 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 177352 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 14974 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 14974 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 16138 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 16138 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 177449 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 177449 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 191702 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 191702 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 61404 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 61404 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 6531 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 6531 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 7193 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 7193 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 1027 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 1027 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 1027 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 145671 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 145671 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 7286 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 7286 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 61399 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 61399 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 155016 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 155016 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 169652 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 169652 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 16211 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 16211 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 121827 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 121827 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 1058 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 1058 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 1058 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 184909 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 184909 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 61398 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 61398 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 156149 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 156149 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 184191 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 184191 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 16133 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 16133 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 187159 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 187159 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 14974 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 14974 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 191470 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 191470 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 16086 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 16086 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 6849 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 6849 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 158538 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 158538 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 6906 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 6906 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 7285 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 7285 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 1022 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 1022 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 1022 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 88638 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 88638 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 88638 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 88638 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 191882 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 191882 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 192343 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 192343 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 188456 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 188456 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 16170 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 16170 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 121810 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 121810 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 7252 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 7252 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 7317 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 7317 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 6391 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 6391 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 16170 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 16170 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 54965 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 54965 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 54965 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 196742 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 196742 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 54965 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 54965 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 54965 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 61396 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 61396 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 14975 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 14975 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 2548 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 16227 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 16227 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 61403 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 61403 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 6680 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 6680 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 7227 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 7227 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 157004 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 157004 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 154248 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 154248 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 178201 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 178201 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 184180 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 184180 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 14979 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 14979 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 191702 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 191702 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 191989 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 191989 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 1152 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 1152 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 1152 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 14973 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 14973 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 184153 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 184153 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 16226 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 16226 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 184813 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 184813 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 6681 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 6681 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 178131 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 178131 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 177730 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 177730 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 6684 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 6684 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 7040 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 7040 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 177554 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 177554 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 171949 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 171949 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 14980 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 14980 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 16112 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 16112 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 178131 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 178131 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 89399 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 89399 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 61450 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 61450 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 14976 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 14976 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 194829 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 194829 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 194829 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 14975 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 14975 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 94657 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 94657 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 121817 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 121817 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 193100 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 193100 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 61451 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 61451 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 121830 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 121830 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 189063 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 189063 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 94682 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 94682 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 184287 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 184287 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 14979 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 14979 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 6934 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 6934 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 194941 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 194941 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 194941 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 177317 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 177317 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 16192 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 16192 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 94656 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 94656 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 159487 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 159487 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 121828 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 121828 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 184910 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 184910 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 177797 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 177797 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 15591 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 15591 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 16172 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 16172 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 88735 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 88735 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 88735 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 88735 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 178068 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 178068 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 193100 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 193100 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 14977 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 14977 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 184180 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 184180 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 7259 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 7259 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 156321 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 156321 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 14972 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 14972 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 14977 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 14977 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 16135 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 16135 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 94632 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 94632 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 192007 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 192007 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 188384 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 188384 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 7101 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 7101 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 7159 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 7159 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 89400 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 89400 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 7422 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 7422 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 188288 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 188288 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 178186 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 178186 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 196379 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 196379 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 184153 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 184153 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 16193 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 16193 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 6745 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 6745 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 155922 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 155922 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 7016 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 7016 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 159350 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 159350 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 157851 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 157851 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 121811 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 121811 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 178068 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 178068 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 88639 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 88639 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 94683 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 94683 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 188456 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 188456 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 158543 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 158543 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 184178 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 184178 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 192091 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 192091 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 6600 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 6600 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 7524 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 7524 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 14976 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 14976 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 192303 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 192303 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 7421 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 7421 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 192342 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 192342 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 178074 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 178074 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 171949 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 171949 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 7314 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 7314 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 7246 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 7246 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 157856 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 157856 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 121807 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 121807 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 121815 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 121815 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 112533 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 112533 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 16171 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 16171 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 88736 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 88736 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 186983 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 186983 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 158760 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 158760 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 88539 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 88539 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 7376 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 7376 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 187043 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 187043 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 184812 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 184812 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 189063 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 189063 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 188734 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 188734 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 186947 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 186947 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 14980 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 14980 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 184157 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 184157 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 7245 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 7245 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 166956 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 166956 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 7287 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 7287 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 184411 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 184411 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 184161 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 184161 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 157632 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 157632 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 121818 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 121818 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 156656 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 156656 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 194829 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 194829 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 194829 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 16132 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 16132 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 16137 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 16137 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 184162 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 184162 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 14972 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 14972 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 159022 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 159022 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 1144 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 1144 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 1144 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 177919 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 177919 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 88539 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 88539 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 88539 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 88539 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 89491 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 89491 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 184217 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 184217 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 184824 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 184824 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 6969 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 6969 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 7524 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 7524 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 61446 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 61446 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 191991 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 191991 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 191991 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 191991 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 157279 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 157279 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 194941 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 194941 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 194941 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 16086 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 16086 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 178070 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 178070 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 14981 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 14981 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 184823 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 184823 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 61401 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 61401 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 177778 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 177778 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 188734 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 188734 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 16213 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 16213 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 61400 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 61400 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 7377 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 7377 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 184821 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 184821 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 6606 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 6606 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 192342 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 192342 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 16214 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 16214 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 16212 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 16212 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 16088 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 16088 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 16228 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 16228 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 1144 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 1144 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 1144 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 16173 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 16173 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 7100 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 7100 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 196055 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 196055 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 145951 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 145951 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 177675 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 177675 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 191470 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 191470 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 16175 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 16175 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 184161 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 184161 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 16113 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 16113 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 7103 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 7103 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 7199 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 7199 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 184216 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 184216 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 192236 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 192236 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 61448 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 61448 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 16210 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 16210 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 195833 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 195833 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 184823 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 184823 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 89490 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 89490 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 177030 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 177030 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 6601 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 6601 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 191782 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 191782 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 188384 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 188384 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 14981 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 14981 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 187044 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 187044 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 94631 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 94631 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 177468 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 177468 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 121813 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 121813 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 159263 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 159263 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 7038 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 7038 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 155017 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 155017 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 121829 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 121829 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 89622 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 89622 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 89622 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 89622 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 156241 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 156241 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 16111 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 16111 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 7415 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 7415 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 184179 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 184179 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 7017 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 7017 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 7375 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 7375 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 89491 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 89491 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 189063 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 189063 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 194829 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 194829 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 194829 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 16209 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 16209 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 191782 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 191782 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 178081 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 178081 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 16193 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 16193 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 16191 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 16191 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 16210 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 16210 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 177030 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 177030 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 94450 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 94450 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 159267 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 159267 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 195842 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 195842 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 156911 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 156911 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 16115 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 16115 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 154391 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 154391 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 188288 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 188288 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 7099 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 7099 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 6842 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 6842 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 7162 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 7162 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 188879 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 188879 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 188879 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 188879 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 191991 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 191991 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 191991 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 191991 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 178104 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 178104 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 7227 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 7227 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 157011 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 157011 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 157772 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 157772 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 184181 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 184181 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 94655 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 94655 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 121809 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 121809 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 7315 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 7315 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 184821 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 184821 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 94748 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 94748 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 88682 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 88682 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 192570 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 192570 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 7338 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 7338 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 7374 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 7374 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 184118 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 184118 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 7215 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 7215 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 189063 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 189063 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 191991 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 191991 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 191991 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 191991 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 191882 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 191882 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 14978 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 14978 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 121808 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 121808 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 94044 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 94044 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 184311 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 184311 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 121814 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 121814 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 16114 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 16114 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 7039 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 7039 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 194829 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 194829 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 194829 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 184181 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 184181 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 121816 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 121816 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 16174 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 16174 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 187178 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 187178 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 154723 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 154723 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 184311 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 184311 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 158707 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 158707 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 6530 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 6530 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 88681 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 88681 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 6672 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 6672 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 6843 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 6843 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 194941 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 194941 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 194941 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 14978 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 14978 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 192343 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 192343 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 192007 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 192007 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 121819 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 121819 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 7158 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 7158 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 16134 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 16134 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 6684 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 6684 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 88639 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 88639 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 121812 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 121812 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 177133 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 177133 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 14973 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 14973 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 6987 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 6987 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 61701 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 61701 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 61747 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 61747 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 7616 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 7616 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 7438 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 7438 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 6920 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 6920 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 89491 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 89491 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 93751 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 93751 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 6921 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 6921 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 3005 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 3005 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 3005 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 3005 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 101592 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 101592 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 89876 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 89876 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 7524 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 7524 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 18938 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 18938 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 18938 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 18938 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 19409 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 19409 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 2591 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 2591 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 2591 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 2591 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 19147 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 19147 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 18840 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 18840 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 7629 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 7629 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 7437 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 7437 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 7437 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 7437 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 61750 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 61750 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 6921 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 6921 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 61705 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 61705 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 6920 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 6920 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 7524 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 7524 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 116910 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 116910 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 61745 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 61745 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 116910 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 116910 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 7616 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 7616 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 118557 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 118557 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 118452 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 118452 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 2560 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 2560 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 2560 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 2560 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 7437 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 7437 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 89491 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 89491 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 61700 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 61700 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 61702 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 61702 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 939 111 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 939 111 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 939 111 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 149257 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 149257 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 2548 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 2548 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 2548 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 2548 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 61752 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 61752 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 61746 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 61746 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 18956 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 18956 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 2560 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 2560 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 2560 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 2560 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 19403 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 19403 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 116837 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 116837 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 7629 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 7629 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 18516 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 18516 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 89928 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 89928 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 61704 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 61704 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 93863 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 93863 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 131 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 131 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 131 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 61703 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 61703 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 7437 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 7437 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 61751 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 61751 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 6987 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 6987 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 61749 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 61749 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 7438 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 7438 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 61748 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 61748 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 217740 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2823 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 2591 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 2591 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 2591 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 2591 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 2560 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 2560 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 2560 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 2560 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 131 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 131 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 131 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