Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
11715531 95472 21 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 5 2 4 1.9 C=CCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL236013 95472 21 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 5 2 4 1.9 C=CCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
28400380 96692 4 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 5 2 3 2.0 CCCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237945 96692 4 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 5 2 3 2.0 CCCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11415838 143135 0 None -1 2 Human 5.0 pEC50 = 5.0 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 316 2 1 4 2.6 Cc1sc(C2(C)OC(C(=O)O)=CC2=O)cc1Br 10.1021/jm070022x
CHEMBL373484 143135 0 None -1 2 Human 5.0 pEC50 = 5.0 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
28400046 96585 3 None 32 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 1.8 CC(C)CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237737 96585 3 None 32 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b 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
10198518 80312 30 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 231 2 1 4 2.2 O=C(O)c1ccc2c(c1)nnn2C1CCCC1 10.1021/jm051099t
CHEMBL201724 80312 30 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 231 2 1 4 2.2 O=C(O)c1ccc2c(c1)nnn2C1CCCC1 10.1021/jm051099t
24955646 64808 0 None -186 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 64808 0 None -186 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
1591 6919 63 None -33 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
6485181 6919 63 None -33 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
CHEMBL428730 6919 63 None -33 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
28400196 97027 19 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 266 7 1 4 2.9 CCCN(CCC)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL238376 97027 19 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 266 7 1 4 2.9 CCCN(CCC)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
44433532 159188 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 2 2 4 0.3 CCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL397055 159188 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
11219885 90237 0 None -3 2 Human 4.9 pEC50 = 4.9 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.5 CC1(c2cccc(C(F)(F)F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL220001 90237 0 None -3 2 Human 4.9 pEC50 = 4.9 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
15604642 82029 0 None -323 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036948 82029 0 None -323 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
43131474 158420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 208 4 2 3 2.2 CC(C)C(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL396382 158420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 208 4 2 3 2.2 CC(C)C(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11961288 203489 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 313 6 2 4 3.4 O=C(O)c1cc(N(Cc2ccccc2)Cc2ccsc2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL564914 203489 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 313 6 2 4 3.4 O=C(O)c1cc(N(Cc2ccccc2)Cc2ccsc2)[nH]n1 10.1016/j.bmcl.2009.05.108
15604637 82035 0 None -70 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036955 82035 0 None -70 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
11380943 90234 1 None -20 2 Human 4.9 pEC50 = 4.9 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL219980 90234 1 None -20 2 Human 4.9 pEC50 = 4.9 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
45269912 202689 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 O=C(O)c1cc(N(Cc2ccsc2)Cc2cccs2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL559204 202689 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 O=C(O)c1cc(N(Cc2ccsc2)Cc2cccs2)[nH]n1 10.1016/j.bmcl.2009.05.108
11687485 96824 4 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 254 6 2 5 1.7 COCC(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL238164 96824 4 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 254 6 2 5 1.7 COCC(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
11483496 6914 0 None -14 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
1589 6914 0 None -14 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
CHEMBL375493 6914 0 None -14 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
11483496 6914 0 None -14 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1589 6914 0 None -14 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL375493 6914 0 None -14 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
28400406 96693 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 208 6 2 3 2.4 CCCCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237946 96693 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 208 6 2 3 2.4 CCCCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11528819 152284 23 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 5 2 4 2.5 CCC(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL391473 152284 23 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 5 2 4 2.5 CCC(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
2829816 95522 54 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 6 2 4 2.5 CCCCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL236219 95522 54 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 6 2 4 2.5 CCCCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
17965902 96589 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 242 3 2 3 2.0 O=C(O)c1ccc(NC(=O)c2ccccc2)nc1 10.1016/j.bmcl.2007.09.058
CHEMBL237739 96589 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 242 3 2 3 2.0 O=C(O)c1ccc(NC(=O)c2ccccc2)nc1 10.1016/j.bmcl.2007.09.058
11379903 91046 0 None -6 2 Human 4.8 pEC50 = 4.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 91046 0 None -6 2 Human 4.8 pEC50 = 4.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
43271548 97031 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 1 3 1.6 CCCN(C)c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL238387 97031 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 1 3 1.6 CCCN(C)c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11379903 91046 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 91046 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11379903 91046 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm800896z
CHEMBL221282 91046 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b 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
11436345 6931 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1599 6931 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL424938 6931 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11218626 91667 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1csc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL223623 91667 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
13153555 100638 27 None -42 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL247921 100638 27 None -42 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
15605571 82010 2 None -23 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 82010 2 None -23 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11470798 144745 1 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)c(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL376419 144745 1 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
283475 96580 118 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 196 3 2 4 1.3 CNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL237731 96580 118 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 196 3 2 4 1.3 CNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
11528793 95477 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 236 4 2 4 2.3 O=C(O)c1ccc(NC2CCC2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
CHEMBL236028 95477 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 236 4 2 4 2.3 O=C(O)c1ccc(NC2CCC2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
10263467 147672 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 235 4 1 5 1.3 COCC(C)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL382096 147672 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 235 4 1 5 1.3 COCC(C)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
2776549 80166 82 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 177 1 1 4 0.7 Cn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL201513 80166 82 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 177 1 1 4 0.7 Cn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
3684804 97025 48 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 210 3 1 4 1.4 CN(C)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL238374 97025 48 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 210 3 1 4 1.4 CN(C)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
11322738 143544 1 None -13 2 Human 4.7 pEC50 = 4.7 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 252 2 1 3 2.1 CC1(c2cccc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL374111 143544 1 None -13 2 Human 4.7 pEC50 = 4.7 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
3729086 152375 58 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 210 4 2 4 1.7 CCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL391547 152375 58 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 210 4 2 4 1.7 CCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
10465474 147235 27 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 203 2 1 4 1.5 O=C(O)c1ccc2c(c1)nnn2C1CC1 10.1021/jm051099t
CHEMBL380939 147235 27 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 203 2 1 4 1.5 O=C(O)c1ccc2c(c1)nnn2C1CC1 10.1021/jm051099t
11322761 148384 1 None -1 2 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)cc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL385103 148384 1 None -1 2 Human 4.6 pEC50 = 4.6 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
3824366 96283 57 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 258 4 2 4 3.0 O=C(O)c1ccc(Nc2ccccc2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
3953363 96283 57 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 258 4 2 4 3.0 O=C(O)c1ccc(Nc2ccccc2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
CHEMBL237296 96283 57 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 258 4 2 4 3.0 O=C(O)c1ccc(Nc2ccccc2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
45269046 203166 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 O=C(O)c1cc(N(Cc2cccs2)Cc2cccs2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL562675 203166 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 O=C(O)c1cc(N(Cc2cccs2)Cc2cccs2)[nH]n1 10.1016/j.bmcl.2009.05.108
11708383 95294 36 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 224 4 2 4 2.1 CC(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL235144 95294 36 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 224 4 2 4 2.1 CC(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
10421571 81000 2 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 235 5 1 5 1.2 CCOCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL202351 81000 2 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 235 5 1 5 1.2 CCOCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
10398515 142069 33 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 219 1 1 4 1.9 CC(C)(C)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL372727 142069 33 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 219 1 1 4 1.9 CC(C)(C)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
28400056 159002 1 None 74 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 208 5 2 3 2.4 CCC(CC)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL396879 159002 1 None 74 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b 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
11276453 91651 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1ccc(C2(C)OC(C(=O)O)=CC2=O)s1 10.1021/jm070022x
CHEMBL223566 91651 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11492560 95293 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 252 7 2 4 2.9 CCCCCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL235141 95293 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 252 7 2 4 2.9 CCCCCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
10014206 79815 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 233 5 1 4 2.3 CCCCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL201048 79815 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 233 5 1 4 2.3 CCCCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
11715556 6908 40 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 224 5 2 4 2.1 CCCNc1ccc(cc1[N+](=O)[O-])C(=O)O 10.1016/j.bmcl.2007.09.058
5801 6908 40 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 224 5 2 4 2.1 CCCNc1ccc(cc1[N+](=O)[O-])C(=O)O 10.1016/j.bmcl.2007.09.058
CHEMBL236011 6908 40 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 224 5 2 4 2.1 CCCNc1ccc(cc1[N+](=O)[O-])C(=O)O 10.1016/j.bmcl.2007.09.058
44250176 7915 0 None 2951 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
5800 7915 0 None 2951 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
CHEMBL564300 7915 0 None 2951 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b 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
51346919 64617 6 None -100 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 64617 6 None -100 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
1595 7047 49 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
51576 7047 49 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
CHEMBL278488 7047 49 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
10353934 139939 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 233 4 1 4 2.5 CCC(CC)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL370386 139939 2 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 233 4 1 4 2.5 CCC(CC)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
10422270 80147 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 251 5 1 5 1.9 CCSCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL201409 80147 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 251 5 1 5 1.9 CCSCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
4992776 97015 33 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 4 2 4 1.9 O=C(O)c1ccc(NC2CC2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
CHEMBL238358 97015 33 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 4 2 4 1.9 O=C(O)c1ccc(NC2CC2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
11565047 153996 25 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 250 4 2 4 2.6 O=C(O)c1ccc(NC2CCCC2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
CHEMBL392830 153996 25 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 250 4 2 4 2.6 O=C(O)c1ccc(NC2CCCC2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
2942936 156643 19 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 266 5 2 5 1.9 O=C(O)c1ccc(NCC2CCCO2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
CHEMBL394906 156643 19 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 266 5 2 5 1.9 O=C(O)c1ccc(NCC2CCCO2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
44434363 175750 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 286 4 2 4 2.5 O=C(O)c1ccc(NC(=O)c2ccccc2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
CHEMBL439028 175750 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 286 4 2 4 2.5 O=C(O)c1ccc(NC(=O)c2ccccc2)c([N+](=O)[O-])c1 10.1016/j.bmcl.2007.09.058
10330955 175884 3 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 217 2 1 4 1.9 O=C(O)c1ccc2c(c1)nnn2C1CCC1 10.1021/jm051099t
CHEMBL440041 175884 3 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 217 2 1 4 1.9 O=C(O)c1ccc2c(c1)nnn2C1CCC1 10.1021/jm051099t
10398583 80744 13 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 221 4 1 5 0.8 COCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL202157 80744 13 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 221 4 1 5 0.8 COCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
28400038 95384 36 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 178 3 2 3 1.4 O=C(O)c1ccc(NC2CC2)nc1 10.1016/j.bmcl.2007.09.058
CHEMBL235615 95384 36 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 178 3 2 3 1.4 O=C(O)c1ccc(NC2CC2)nc1 10.1016/j.bmcl.2007.09.058
44433529 95311 0 None 5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 176 2 2 4 0.5 c1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
CHEMBL235230 95311 0 None 5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
2771812 96586 53 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 214 3 2 3 2.5 O=C(O)c1ccc(Nc2ccccc2)nc1 10.1016/j.bmcl.2007.09.058
CHEMBL237738 96586 53 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 214 3 2 3 2.5 O=C(O)c1ccc(Nc2ccccc2)nc1 10.1016/j.bmcl.2007.09.058
43187344 97029 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 210 5 2 4 1.2 COCC(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL238385 97029 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 210 5 2 4 1.2 COCC(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11817645 91681 1 None -12 2 Human 4.5 pEC50 = 4.5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2cc(F)cc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223700 91681 1 None -12 2 Human 4.5 pEC50 = 4.5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
10013684 80804 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 219 3 1 4 2.1 CCC(C)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL202206 80804 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 219 3 1 4 2.1 CCC(C)n1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
4712703 148000 44 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 204 2 1 3 2.3 CC(C)n1cnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL382863 148000 44 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 204 2 1 3 2.3 CC(C)n1cnc2cc(C(=O)O)ccc21 10.1021/jm051099t
44433529 95311 0 None 5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 176 2 2 4 0.5 c1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
CHEMBL235230 95311 0 None 5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
11322762 144380 1 None -5 2 Human 4.4 pEC50 = 4.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2c(F)cccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375625 144380 1 None -5 2 Human 4.4 pEC50 = 4.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
43085192 96206 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 252 5 2 4 2.7 CC(C)C(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL237077 96206 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 252 5 2 4 2.7 CC(C)C(C)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
11483496 6914 0 None -14 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1589 6914 0 None -14 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL375493 6914 0 None -14 2 Human 6.4 pEC50 = 6.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11311474 172561 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2ccc(Cl)s2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL424750 172561 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
43187332 158999 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 2.0 CCC(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL396878 158999 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 2.0 CCC(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
1447952 96584 7 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 206 3 2 3 2.1 O=C(O)c1ccc(NC2CCCC2)nc1 10.1016/j.bmcl.2007.09.058
CHEMBL237735 96584 7 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 206 3 2 3 2.1 O=C(O)c1ccc(NC2CCCC2)nc1 10.1016/j.bmcl.2007.09.058
11744994 96581 26 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 166 3 2 3 1.2 CCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237732 96581 26 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 166 3 2 3 1.2 CCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
1597 8746 80 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm051099t
2736690 8746 80 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm051099t
CHEMBL381638 8746 80 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm051099t
45268162 203018 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 235 6 2 3 1.7 O=C(O)c1cc(N(CC2CC2)CC2CC2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL561720 203018 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 235 6 2 3 1.7 O=C(O)c1cc(N(CC2CC2)CC2CC2)[nH]n1 10.1016/j.bmcl.2009.05.108
28399894 156066 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 178 4 2 3 1.4 C=CCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2009.05.108
CHEMBL394468 156066 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 178 4 2 3 1.4 C=CCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2009.05.108
11324121 91441 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 CC1(c2cc(Br)cs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222472 91441 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
776421 96703 108 None -30 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL238002 96703 108 None -30 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
1595 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
51576 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
CHEMBL278488 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
1595 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
51576 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
CHEMBL278488 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11183678 91547 1 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2ccsc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223140 91547 1 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
1595 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
51576 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
CHEMBL278488 7047 49 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109b 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
11992587 202277 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 183 4 3 3 1.3 CCC(C)Nc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2009.05.108
CHEMBL553415 202277 1 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 183 4 3 3 1.3 CCC(C)Nc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2009.05.108
11148966 7906 4 None 4 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
1598 7906 4 None 4 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
CHEMBL436301 7906 4 None 4 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11380943 90234 1 None -20 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL219980 90234 1 None -20 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11436345 6931 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1599 6931 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL424938 6931 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
9971057 81078 4 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 283 4 1 5 2.2 COc1cccc(Cn2nnc3cc(C(=O)O)ccc32)c1 10.1021/jm051099t
CHEMBL202427 81078 4 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 283 4 1 5 2.2 COc1cccc(Cn2nnc3cc(C(=O)O)ccc32)c1 10.1021/jm051099t
28399946 96582 8 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 180 4 2 3 1.6 CCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237733 96582 8 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 180 4 2 3 1.6 CCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11739420 91532 0 None -12 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 344 2 1 3 2.1 CC1(c2cccc(I)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223013 91532 0 None -12 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
11413114 144397 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 3 1.4 CC1(C2=CCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375754 144397 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
43271417 97026 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 5 1 4 2.1 CCCN(C)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL238375 97026 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 5 1 4 2.1 CCCN(C)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
11992688 202518 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 335 8 2 3 3.4 O=C(O)c1cc(N(CCc2ccccc2)CCc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL557298 202518 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 335 8 2 3 3.4 O=C(O)c1cc(N(CCc2ccccc2)CCc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
11514348 159868 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 252 6 2 4 2.9 CCC(CC)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL397616 159868 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 252 6 2 4 2.9 CCC(CC)Nc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
4738197 158084 39 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 240 6 2 5 1.4 COCCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL396073 158084 39 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 240 6 2 5 1.4 COCCNc1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
653819 148039 50 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 245 2 1 4 2.6 O=C(O)c1ccc2c(c1)nnn2C1CCCCC1 10.1021/jm051099t
CHEMBL383099 148039 50 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 245 2 1 4 2.6 O=C(O)c1ccc2c(c1)nnn2C1CCCCC1 10.1021/jm051099t
59343664 82031 0 None -29 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 82031 0 None -29 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
43187366 97030 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 4 2 4 1.4 O=C(O)c1ccc(NCC2CCCO2)nc1 10.1016/j.bmcl.2007.09.058
CHEMBL238386 97030 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 4 2 4 1.4 O=C(O)c1ccc(NCC2CCCO2)nc1 10.1016/j.bmcl.2007.09.058
28400003 156068 37 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 180 3 2 3 1.6 CC(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL394469 156068 37 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 180 3 2 3 1.6 CC(C)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
11184165 90229 0 None -5 2 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 246 3 1 3 2.0 CCc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL219950 90229 0 None -5 2 Human 5.2 pEC50 = 5.2 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
2833647 156646 24 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 5 1 4 2.1 CCN(CC)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
CHEMBL394907 156646 24 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 238 5 1 4 2.1 CCN(CC)c1ccc(C(=O)O)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.058
16775596 96386 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 6 1 3 2.4 CCCN(CCC)c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237525 96386 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 222 6 1 3 2.4 CCCN(CCC)c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
59304608 82034 0 None -67 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 82034 0 None -67 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
11992588 202228 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 197 5 3 3 1.7 CCCC(C)Nc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2009.05.108
CHEMBL552399 202228 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 197 5 3 3 1.7 CCCC(C)Nc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2009.05.108
11379903 91046 0 None -6 2 Human 6.2 pEC50 = 6.2 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 91046 0 None -6 2 Human 6.2 pEC50 = 6.2 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
10331019 81188 31 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 219 4 1 4 1.9 CCCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL202586 81188 31 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 219 4 1 4 1.9 CCCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
28399894 156066 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 178 4 2 3 1.4 C=CCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL394468 156066 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 178 4 2 3 1.4 C=CCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
44434380 96385 21 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 192 3 2 3 1.7 O=C(O)c1ccc(NC2CCC2)nc1 10.1016/j.bmcl.2007.09.058
CHEMBL237524 96385 21 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 192 3 2 3 1.7 O=C(O)c1ccc(NC2CCC2)nc1 10.1016/j.bmcl.2007.09.058
44433528 154300 0 None 10 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 3 2 4 0.5 CCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393064 154300 0 None 10 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
22271415 95299 57 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 152 2 2 3 0.8 CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL235168 95299 57 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 152 2 2 3 0.8 CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
10058774 81192 28 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 205 3 1 4 1.5 CCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL202614 81192 28 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 205 3 1 4 1.5 CCCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
44433530 154302 0 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 192 4 2 4 0.9 CCCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393065 154302 0 None 2 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
117629482 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
1588 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
1594 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
2835 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
938 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
CHEMBL573 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
DB00627 9599 140 None -26 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109b 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
11992592 202810 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 211 6 2 3 1.7 CCCN(CCC)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2009.05.108
CHEMBL560254 202810 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 211 6 2 3 1.7 CCCN(CCC)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2009.05.108
11992591 203049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 307 6 2 3 3.3 O=C(O)c1cc(N(Cc2ccccc2)Cc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL561920 203049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 307 6 2 3 3.3 O=C(O)c1cc(N(Cc2ccccc2)Cc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
11992790 201971 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b 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(Cc2ccccc2F)Cc2ccccc2F)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL550563 201971 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b 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(Cc2ccccc2F)Cc2ccccc2F)[nH]n1 10.1016/j.bmcl.2009.05.108
2103992 175905 46 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 191 2 1 4 1.1 CCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
CHEMBL440217 175905 46 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 191 2 1 4 1.1 CCn1nnc2cc(C(=O)O)ccc21 10.1021/jm051099t
45269904 203511 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 287 6 2 5 2.5 O=C(O)c1cc(N(Cc2ccoc2)Cc2ccoc2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL565055 203511 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109b receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 287 6 2 5 2.5 O=C(O)c1cc(N(Cc2ccoc2)Cc2ccoc2)[nH]n1 10.1016/j.bmcl.2009.05.108
11608532 80069 31 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 253 3 1 4 2.2 O=C(O)c1ccc2c(c1)nnn2Cc1ccccc1 10.1021/jm051099t
CHEMBL201278 80069 31 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonistic activity at GPR109b by cAMP whole cell assayAgonistic activity at GPR109b by cAMP whole cell assay
ChEMBL 253 3 1 4 2.2 O=C(O)c1ccc2c(c1)nnn2Cc1ccccc1 10.1021/jm051099t
28400019 95341 9 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 196 5 2 4 0.8 COCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL235394 95341 9 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109b receptor transfected in CHOK1 cells assessed as reversal of forskolin-induced cAMP elevating effect by whole cell assay
ChEMBL 196 5 2 4 0.8 COCCNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
56950369 10332 13 None -47 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 10332 13 None -47 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 10332 13 None -47 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 10332 13 None -47 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR109bAgonist activity at human GPR109b
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
11264843 144398 1 None -1 2 Human 5.0 pEC50 = 5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccc(F)cc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375762 144398 1 None -1 2 Human 5.0 pEC50 = 5 Functional
Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109b 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
1595 7047 49 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
51576 7047 49 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
CHEMBL278488 7047 49 None -4 2 Human 5.5 pIC50 = 5.5 Functional
Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
117629482 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 9599 140 None -26 4 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
5798 8284 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@@H](Cc1c[nH]c2c1cccc2)N 19237584
6923517 8284 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@@H](Cc1c[nH]c2c1cccc2)N 19237584
9060 8284 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@@H](Cc1c[nH]c2c1cccc2)N 19237584
CHEMBL292303 8284 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@@H](Cc1c[nH]c2c1cccc2)N 19237584
DB03225 8284 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@@H](Cc1c[nH]c2c1cccc2)N 19237584
5797 8257 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 0.6 N[C@@H](C(=O)O)Cc1ccccc1 19237584
6919011 8257 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 0.6 N[C@@H](C(=O)O)Cc1ccccc1 19237584
71567 8257 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 0.6 N[C@@H](C(=O)O)Cc1ccccc1 19237584
CHEMBL379630 8257 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 0.6 N[C@@H](C(=O)O)Cc1ccccc1 19237584
DB02556 8257 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 0.6 N[C@@H](C(=O)O)Cc1ccccc1 19237584
11367166 6889 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 6 2 2 1.4 CCCCC[C@@H](CC(=O)O)O 19561068
2933 6889 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 6 2 2 1.4 CCCCC[C@@H](CC(=O)O)O 19561068
117629482 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1588 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1594 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
2835 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
938 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
CHEMBL573 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
DB00627 9599 140 None -26 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
5796 6855 77 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 19561068
94180 6855 77 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 19561068
CHEMBL4447980 6855 77 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 6 2 2 1.4 CCCCCCC(C(=O)O)O 19561068
1152206 8222 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 208 4 3 4 0.3 OC(=O)[C@@H](CC(=O)c1ccccc1N)N 19237584
5799 8222 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 208 4 3 4 0.3 OC(=O)[C@@H](CC(=O)c1ccccc1N)N 19237584
6971244 8222 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 208 4 3 4 0.3 OC(=O)[C@@H](CC(=O)c1ccccc1N)N 19237584
CHEMBL1233899 8222 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 208 4 3 4 0.3 OC(=O)[C@@H](CC(=O)c1ccccc1N)N 19237584
1597 8746 80 None -1 2 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 16480258
2736690 8746 80 None -1 2 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 16480258
CHEMBL381638 8746 80 None -1 2 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 16480258
12418 8258 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 166 3 2 2 0.7 C1=CC=C(C=C1)C[C@@H](C(=O)O)O 31120900
444718 8258 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 166 3 2 2 0.7 C1=CC=C(C=C1)C[C@@H](C(=O)O)O 31120900
DB02494 8258 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 166 3 2 2 0.7 C1=CC=C(C=C1)C[C@@H](C(=O)O)O 31120900
11715556 6908 40 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 224 5 2 4 2.1 CCCNc1ccc(cc1[N+](=O)[O-])C(=O)O 17931863
5801 6908 40 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 224 5 2 4 2.1 CCCNc1ccc(cc1[N+](=O)[O-])C(=O)O 17931863
CHEMBL236011 6908 40 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 224 5 2 4 2.1 CCCNc1ccc(cc1[N+](=O)[O-])C(=O)O 17931863
44250176 7915 0 None 2951 2 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 19524438
5800 7915 0 None 2951 2 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 19524438
CHEMBL564300 7915 0 None 2951 2 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 19524438
1595 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
1595 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
1595 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
1595 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
51576 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
51576 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
51576 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
51576 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
CHEMBL278488 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
CHEMBL278488 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
CHEMBL278488 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
CHEMBL278488 7047 49 None -4 2 Human 5.0 pEC50 None 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
11148966 7906 4 None 4 2 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 17358052
1598 7906 4 None 4 2 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 17358052
CHEMBL436301 7906 4 None 4 2 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 17358052
11436345 6931 0 None -1 2 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
1599 6931 0 None -1 2 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
CHEMBL424938 6931 0 None -1 2 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
53232 195404 95 None 1 10 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 None
CHEMBL503 195404 95 None 1 10 Human 8.2 pIC50 = 8.2 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




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
1595 7047 49 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
51576 7047 49 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
CHEMBL278488 7047 49 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA3 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
135899171 22942 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of radioligand from human GPR109BDisplacement of radioligand from human GPR109B
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 22942 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of radioligand from human GPR109BDisplacement of radioligand from human GPR109B
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108