Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 59304608 | 75285 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | 3 | 4 | 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 | 75285 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | 3 | 4 | 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 | 7376 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 7376 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 75283 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 75283 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 75288 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 75288 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 162381 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | 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 | 162381 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | 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 | 162381 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | 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 | 162381 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | 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 | 177135 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 177135 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 93762 | None | 59 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 93762 | None | 59 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | 6747 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 6747 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 7 | 7.0 | -4 | 4 | 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 | 177780 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 177780 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | None | 82 | Human | Functional | pEC50 | = | 6 | 6.0 | -4 | 4 | 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 | 88672 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 88672 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | ||
Showing 1 to 50 of 1,508 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 1596 | 260 | None | 60 | Human | Binding | pAC50 | = | 5.4 | 5.4 | - | 0 | 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 | None | 60 | Human | Binding | pAC50 | = | 5.4 | 5.4 | - | 0 | 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 | None | 60 | Human | Binding | pAC50 | = | 5.4 | 5.4 | - | 0 | 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 | None | 60 | Human | Binding | pAC50 | = | 5.4 | 5.4 | - | 0 | 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 | None | 60 | Human | Binding | pAC50 | = | 5.4 | 5.4 | - | 0 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 6 | 6.0 | -3 | 2 | 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 | 7317 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 7317 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 6686 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 6686 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 177753 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | 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 | 177753 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | 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 | 177766 | None | 4 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 177766 | None | 4 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 6532 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 6532 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 89656 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 89656 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | None | 82 | Human | Binding | pEC50 | = | 7.8 | 7.8 | -3 | 2 | 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 | 178320 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 178320 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | None | 36 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | None | 36 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | None | 36 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 178029 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 178029 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 178079 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 178079 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 6908 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 6908 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 6851 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 6851 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 177503 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | 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 | 177503 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | 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 | 7103 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | 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 | 7103 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | 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 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | 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 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | 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 | ||
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