Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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
11433866 20999 4 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 607 8 7 14 -0.2 Nc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1097652 20999 4 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 607 8 7 14 -0.2 Nc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1199140 20999 4 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 607 8 7 14 -0.2 Nc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
44755067 20997 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 575 10 7 14 0.1 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm901691y
CHEMBL1096742 20997 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 575 10 7 14 0.1 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm901691y
CHEMBL1199118 20997 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 575 10 7 14 0.1 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm901691y
46222216 21001 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 554 9 7 13 0.1 CNc1nc(Cl)cc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1098419 21001 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 554 9 7 13 0.1 CNc1nc(Cl)cc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1199150 21001 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 554 9 7 13 0.1 CNc1nc(Cl)cc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
145978218 170339 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 353 9 3 3 4.1 CCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4203088 170339 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 353 9 3 3 4.1 CCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
46222214 21013 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 555 9 7 14 -0.5 CNc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1098083 21013 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 555 9 7 14 -0.5 CNc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1199366 21013 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 555 9 7 14 -0.5 CNc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
446916 112902 72 None -9 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL31344 112902 72 None -9 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL3264006 112902 72 None -9 3 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
146015339 10694 32 None -3 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901691y
1749 10694 32 None -3 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901691y
6031 10694 32 None -3 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901691y
CHEMBL130266 10694 32 None -3 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901691y
DB03435 10694 32 None -3 7 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901691y
145977144 170624 0 None 45 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 333 10 3 3 3.8 CCCCCCOc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4206497 170624 0 None 45 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 333 10 3 3 3.8 CCCCCCOc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
145964032 170841 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 395 12 3 3 5.3 CCCCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4209219 170841 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 395 12 3 3 5.3 CCCCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
71280866 112789 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 389 4 3 2 3.4 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(Br)c12 nan
CHEMBL3132880 112789 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 389 4 3 2 3.4 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(Br)c12 nan
71281465 150132 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 261 4 3 2 2.5 Cc1cc(C)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 nan
CHEMBL3897541 150132 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 261 4 3 2 2.5 Cc1cc(C)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 nan
71281224 171592 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 317 5 3 3 3.3 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(-c3ccco3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4218582 171592 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 317 5 3 3 3.3 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(-c3ccco3)ccc12 10.1021/acs.jmedchem.7b01768
145972331 171380 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 377 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(I)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4215819 171380 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 377 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(I)c12 10.1021/acs.jmedchem.7b01768
71281465 150132 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 261 4 3 2 2.5 Cc1cc(C)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL3897541 150132 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 261 4 3 2 2.5 Cc1cc(C)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
15747650 201596 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 269 4 3 2 2.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(F)c12 nan
CHEMBL53914 201596 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 269 4 3 2 2.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(F)c12 nan
CHEMBL5086989 221840 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Inverse agonist at human GPR17 in human LN-229 cells assessed as intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assayInverse agonist at human GPR17 in human LN-229 cells assessed as intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assay
ChEMBL None None None O=C(O)CCC1=C(C(=O)O)Cc2cc(Cl)cc(Cl)c21 10.1021/acs.jmedchem.1c00277
96412014 170871 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 257 3 2 1 3.5 O=C(O)CCc1c[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4209578 170871 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 257 3 2 1 3.5 O=C(O)CCc1c[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
76311173 112791 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 369 4 3 2 3.9 O=C(O)CCc1c(C(=O)O)[nH]c2cc(C(F)(F)F)cc(C(F)(F)F)c12 10.1039/C3MD00309D
CHEMBL3132882 112791 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 369 4 3 2 3.9 O=C(O)CCc1c(C(=O)O)[nH]c2cc(C(F)(F)F)cc(C(F)(F)F)c12 10.1039/C3MD00309D
CHEMBL5086989 221840 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Inverse agonist at human GPR17 in human SNB-19 cells assessed as intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assayInverse agonist at human GPR17 in human SNB-19 cells assessed as intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assay
ChEMBL None None None O=C(O)CCC1=C(C(=O)O)Cc2cc(Cl)cc(Cl)c21 10.1021/acs.jmedchem.1c00277
71280744 153136 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 373 7 3 4 3.1 O=C(O)CCc1c(C(=O)O)n(CCC(=O)O)c2cc(Cl)cc(Cl)c12 nan
CHEMBL3921330 153136 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 373 7 3 4 3.1 O=C(O)CCc1c(C(=O)O)n(CCC(=O)O)c2cc(Cl)cc(Cl)c12 nan
CHEMBL5083629 221655 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human GPR17 in human SNB-19 cells assessed as decrease in intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assayAgonist activity at human GPR17 in human SNB-19 cells assessed as decrease in intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assay
ChEMBL None None None O=C(Nc1ccccc1)Oc1cc(OC(=O)Nc2ccccc2)c2c(c1)N(C(c1ccc(F)cc1)c1cccc(Cl)c1O)CC2 10.1021/acs.jmedchem.1c00277
71280866 112789 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 389 4 3 2 3.4 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(Br)c12 nan
CHEMBL3132880 112789 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 389 4 3 2 3.4 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(Br)c12 nan
4052279 107972 8 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)ccc12 nan
CHEMBL295718 107972 8 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)ccc12 nan
71280866 112789 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 389 4 3 2 3.4 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(Br)c12 10.1039/C3MD00309D
CHEMBL3132880 112789 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 389 4 3 2 3.4 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(Br)c12 10.1039/C3MD00309D
22163898 112794 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)ccc12 10.1039/C3MD00309D
CHEMBL3132885 112794 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)ccc12 10.1039/C3MD00309D
145971828 171344 0 None -33 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4215280 171344 0 None -33 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL5086989 221840 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR17 in human SNB-19 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assayAgonist activity at human GPR17 in human SNB-19 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assay
ChEMBL None None None O=C(O)CCC1=C(C(=O)O)Cc2cc(Cl)cc(Cl)c21 10.1021/acs.jmedchem.1c00277
CHEMBL5086989 221840 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human GPR17 in human LN-229 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assayAgonist activity at human GPR17 in human LN-229 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assay
ChEMBL None None None O=C(O)CCC1=C(C(=O)O)Cc2cc(Cl)cc(Cl)c21 10.1021/acs.jmedchem.1c00277
145971655 171443 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 329 4 3 2 2.8 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(F)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4216761 171443 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 329 4 3 2 2.8 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)cc(F)c12 10.1021/acs.jmedchem.7b01768
15747657 195699 6 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 325 6 3 3 3.7 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Oc3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL50784 195699 6 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 325 6 3 3 3.7 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Oc3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
14783467 195165 8 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cccc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL50160 195165 8 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cccc(Cl)c12 10.1021/acs.jmedchem.7b01768
71280863 170605 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 327 5 3 2 3.7 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(-c3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4206322 170605 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 327 5 3 2 3.7 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(-c3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
71281161 152339 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 385 6 3 2 5.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)cc(-c3ccccc3)c12 nan
CHEMBL3915176 152339 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 385 6 3 2 5.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)cc(-c3ccccc3)c12 nan
71281161 152339 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 385 6 3 2 5.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)cc(-c3ccccc3)c12 nan
CHEMBL3915176 152339 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 385 6 3 2 5.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)cc(-c3ccccc3)c12 nan
145971828 171344 0 None -44 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4215280 171344 0 None -44 3 Mouse 5.5 pEC50 = 5.5 Functional
Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
22163898 112794 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)ccc12 nan
CHEMBL3132885 112794 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)ccc12 nan
22163898 112794 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)ccc12 nan
CHEMBL3132885 112794 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Br)ccc12 nan
145978078 170530 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 377 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(F)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4205476 170530 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 377 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(F)c12 10.1021/acs.jmedchem.7b01768
446916 112902 72 None 5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1039/C3MD00309D
CHEMBL31344 112902 72 None 5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1039/C3MD00309D
CHEMBL3264006 112902 72 None 5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1039/C3MD00309D
71281465 150132 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 261 4 3 2 2.5 Cc1cc(C)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 nan
CHEMBL3897541 150132 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 261 4 3 2 2.5 Cc1cc(C)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 nan
145965484 170981 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 361 5 3 2 4.3 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(-c3ccc(F)cc3)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4210864 170981 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 361 5 3 2 4.3 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(-c3ccc(F)cc3)c12 10.1021/acs.jmedchem.7b01768
76314777 112795 1 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cccc(I)c12 10.1039/C3MD00309D
CHEMBL3132886 112795 1 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cccc(I)c12 10.1039/C3MD00309D
4052279 107972 8 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)ccc12 nan
CHEMBL295718 107972 8 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)ccc12 nan
4052279 107972 8 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL295718 107972 8 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 267 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)ccc12 10.1021/acs.jmedchem.7b01768
71280847 170471 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 327 5 3 2 3.7 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccc(F)cc3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4204883 170471 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 327 5 3 2 3.7 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccc(F)cc3)ccc12 10.1021/acs.jmedchem.7b01768
71281161 152339 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 385 6 3 2 5.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)cc(-c3ccccc3)c12 10.1021/acs.jmedchem.7b01768
CHEMBL3915176 152339 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 385 6 3 2 5.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)cc(-c3ccccc3)c12 10.1021/acs.jmedchem.7b01768
71281286 170889 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 299 5 3 3 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccco3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4209766 170889 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 299 5 3 3 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccco3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL5083629 221655 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human GPR17 in human LN-229 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assayAgonist activity at human GPR17 in human LN-229 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assay
ChEMBL None None None O=C(Nc1ccccc1)Oc1cc(OC(=O)Nc2ccccc2)c2c(c1)N(C(c1ccc(F)cc1)c1cccc(Cl)c1O)CC2 10.1021/acs.jmedchem.1c00277
145964575 171029 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 361 5 3 2 4.3 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccc(F)cc3)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4211381 171029 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 361 5 3 2 4.3 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccc(F)cc3)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
22163902 112793 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cccc(Br)c12 10.1039/C3MD00309D
CHEMBL3132884 112793 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 311 4 3 2 2.6 O=C(O)CCc1c(C(=O)O)[nH]c2cccc(Br)c12 10.1039/C3MD00309D
71280939 112790 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 485 4 3 2 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(I)c12 nan
CHEMBL3132881 112790 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 485 4 3 2 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(I)c12 nan
71280939 112790 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 485 4 3 2 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(I)c12 nan
CHEMBL3132881 112790 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 485 4 3 2 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(I)c12 nan
71280939 112790 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 485 4 3 2 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(I)c12 10.1039/C3MD00309D
CHEMBL3132881 112790 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 485 4 3 2 3.1 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)cc(I)c12 10.1039/C3MD00309D
71280760 171055 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 329 4 3 2 2.8 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(Br)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4211793 171055 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 329 4 3 2 2.8 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(Br)ccc12 10.1021/acs.jmedchem.7b01768
71280865 171623 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 323 6 3 2 3.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cc3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4218936 171623 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 323 6 3 2 3.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cc3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
71280882 112792 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 319 4 3 2 3.3 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)c(F)c(Cl)c12 10.1039/C3MD00309D
CHEMBL3132883 112792 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 319 4 3 2 3.3 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)c(F)c(Cl)c12 10.1039/C3MD00309D
71280744 153136 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 373 7 3 4 3.1 O=C(O)CCc1c(C(=O)O)n(CCC(=O)O)c2cc(Cl)cc(Cl)c12 nan
CHEMBL3921330 153136 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 373 7 3 4 3.1 O=C(O)CCc1c(C(=O)O)n(CCC(=O)O)c2cc(Cl)cc(Cl)c12 nan
145977144 170624 0 None -45 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 333 10 3 3 3.8 CCCCCCOc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4206497 170624 0 None -45 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 333 10 3 3 3.8 CCCCCCOc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
71280744 153136 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 373 7 3 4 3.1 O=C(O)CCc1c(C(=O)O)n(CCC(=O)O)c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL3921330 153136 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 373 7 3 4 3.1 O=C(O)CCc1c(C(=O)O)n(CCC(=O)O)c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL5083629 221655 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human GPR17 in human LN-229 cells assessed as decrease in intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assayAgonist activity at human GPR17 in human LN-229 cells assessed as decrease in intracellular cAMP levels incubated for 2 hrs by cAMP Glo Dynamic assay
ChEMBL None None None O=C(Nc1ccccc1)Oc1cc(OC(=O)Nc2ccccc2)c2c(c1)N(C(c1ccc(F)cc1)c1cccc(Cl)c1O)CC2 10.1021/acs.jmedchem.1c00277
446916 112902 72 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 nan
CHEMBL31344 112902 72 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 nan
CHEMBL3264006 112902 72 None 5 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 nan
145971906 171478 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 329 4 3 2 2.8 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(Br)c12 10.1021/acs.jmedchem.7b01768
CHEMBL4217194 171478 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 329 4 3 2 2.8 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(Br)c12 10.1021/acs.jmedchem.7b01768
145971828 171344 0 None 33 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4215280 171344 0 None 33 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
446916 112902 72 None -5 3 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL31344 112902 72 None -5 3 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL3264006 112902 72 None -5 3 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assayAgonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
71280879 112796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)ccc12 nan
CHEMBL3132887 112796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)ccc12 nan
71280879 112796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)ccc12 nan
CHEMBL3132887 112796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)ccc12 nan
71280879 112796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)ccc12 10.1039/C3MD00309D
CHEMBL3132887 112796 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assayAgonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
ChEMBL 359 4 3 2 2.5 O=C(O)CCc1c(C(=O)O)[nH]c2cc(I)ccc12 10.1039/C3MD00309D
71280862 158981 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 309 5 3 2 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)ccc12 nan
CHEMBL3968577 158981 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in CHO cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 309 5 3 2 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)ccc12 nan
71280862 158981 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 309 5 3 2 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)ccc12 nan
CHEMBL3968577 158981 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 309 5 3 2 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)ccc12 nan
71280862 158981 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 309 5 3 2 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL3968577 158981 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 309 5 3 2 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3ccccc3)ccc12 10.1021/acs.jmedchem.7b01768
15747650 201596 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 269 4 3 2 2.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(F)c12 10.1021/acs.jmedchem.7b01768
CHEMBL53914 201596 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 269 4 3 2 2.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(F)c12 10.1021/acs.jmedchem.7b01768
15747650 201596 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 269 4 3 2 2.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(F)c12 nan
CHEMBL53914 201596 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 269 4 3 2 2.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(F)cc(F)c12 nan
CHEMBL5083629 221655 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR17 in human SNB-19 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assayAgonist activity at human GPR17 in human SNB-19 cells assessed as decrease in calcium ion levels incubated for 2 hrs by Calcium Fura 2 Dynamic assay
ChEMBL None None None O=C(Nc1ccccc1)Oc1cc(OC(=O)Nc2ccccc2)c2c(c1)N(C(c1ccc(F)cc1)c1cccc(Cl)c1O)CC2 10.1021/acs.jmedchem.1c00277
71280970 170599 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 285 4 3 2 2.7 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(Cl)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4206245 170599 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 285 4 3 2 2.7 O=C(O)CCc1c(C(=O)O)[nH]c2c(F)c(Cl)ccc12 10.1021/acs.jmedchem.7b01768
446916 112902 72 None 5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 nan
CHEMBL31344 112902 72 None 5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 nan
CHEMBL3264006 112902 72 None 5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assayAgonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 nan
16007361 206093 1 None -43 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 530 6 6 10 -2.0 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm901691y
CHEMBL1094759 206093 1 None -43 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 530 6 6 10 -2.0 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm901691y
CHEMBL4287835 206093 1 None -43 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 530 6 6 10 -2.0 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm901691y
CHEMBL590494 206093 1 None -43 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 530 6 6 10 -2.0 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm901691y
71281217 171554 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 315 5 3 3 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3cccs3)ccc12 10.1021/acs.jmedchem.7b01768
CHEMBL4218030 171554 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAgonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 315 5 3 3 3.6 O=C(O)CCc1c(C(=O)O)[nH]c2cc(-c3cccs3)ccc12 10.1021/acs.jmedchem.7b01768
1776 7574 38 None 2 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 10.1021/jm901691y
5006 7574 38 None 2 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 10.1021/jm901691y
9854012 7574 38 None 2 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 10.1021/jm901691y
CHEMBL334966 7574 38 None 2 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 10.1021/jm901691y
DB06441 7574 38 None 2 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 10.1021/jm901691y
23279502 20992 4 None 169 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 521 9 7 14 -1.2 CNc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1094109 20992 4 None 169 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 521 9 7 14 -1.2 CNc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
CHEMBL1199042 20992 4 None 169 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 521 9 7 14 -1.2 CNc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901691y
162650391 186863 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)cc1 10.1016/j.ejmech.2019.111789
CHEMBL4748101 186863 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)cc1 10.1016/j.ejmech.2019.111789
162652460 187203 0 None 9 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 392 5 1 5 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc(C#N)c3)cc2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4752357 187203 0 None 9 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 392 5 1 5 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc(C#N)c3)cc2)c1 10.1016/j.ejmech.2019.111789
162649995 186893 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 428 7 1 7 3.6 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4748522 186893 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 428 7 1 7 3.6 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)c1 10.1016/j.ejmech.2019.111789
162646428 186456 6 None 3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccccc1Cl 10.1016/j.ejmech.2019.111789
CHEMBL4743510 186456 6 None 3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccccc1Cl 10.1016/j.ejmech.2019.111789
129834484 188816 0 None 1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4780920 188816 0 None 1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)cc2)c1 10.1016/j.ejmech.2019.111789
162643268 188528 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1cccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)c1)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111789
CHEMBL4777444 188528 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1cccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)c1)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111789
1440 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1016/j.ejmech.2019.111789
1909 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1016/j.ejmech.2019.111789
3715 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1016/j.ejmech.2019.111789
CHEMBL6 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1016/j.ejmech.2019.111789
DB00328 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1016/j.ejmech.2019.111789
1440 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.7b01768
1909 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.7b01768
3715 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.7b01768
CHEMBL6 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.7b01768
DB00328 8808 119 None -74 7 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.7b01768
162647196 186437 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111789
CHEMBL4743246 186437 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Cl)c1 10.1016/j.ejmech.2019.111789
162651144 187070 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1cccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)c1)c1ccc(Cl)cc1 10.1016/j.ejmech.2019.111789
CHEMBL4750852 187070 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1cccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)c1)c1ccc(Cl)cc1 10.1016/j.ejmech.2019.111789
162675500 190067 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 398 6 1 6 3.6 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccccc1 10.1016/j.ejmech.2019.111789
CHEMBL4796857 190067 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 398 6 1 6 3.6 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccccc1 10.1016/j.ejmech.2019.111789
162666217 189066 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 466 6 1 6 4.9 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.ejmech.2019.111789
CHEMBL4783980 189066 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 466 6 1 6 4.9 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.ejmech.2019.111789
162653582 187330 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2019.111789
CHEMBL4753843 187330 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 432 6 1 6 4.3 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2019.111789
162676228 190082 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 416 6 1 6 3.8 O=C(Nc1cccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)c1)c1cccc(F)c1 10.1016/j.ejmech.2019.111789
CHEMBL4797060 190082 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 416 6 1 6 3.8 O=C(Nc1cccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)c1)c1cccc(F)c1 10.1016/j.ejmech.2019.111789
162661229 188289 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 466 6 1 6 4.6 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(C(F)(F)F)c1 10.1016/j.ejmech.2019.111789
CHEMBL4764999 188289 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 466 6 1 6 4.6 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(C(F)(F)F)c1 10.1016/j.ejmech.2019.111789
162676436 190260 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 403 5 3 4 4.7 COC(=O)c1cccc(NC(=O)Nc2cccc(NC(=O)c3cccc(C)c3)c2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4799394 190260 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 403 5 3 4 4.7 COC(=O)c1cccc(NC(=O)Nc2cccc(NC(=O)c3cccc(C)c3)c2)c1 10.1016/j.ejmech.2019.111789
162646235 186294 0 None 2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 476 6 1 6 4.4 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Br)c1 10.1016/j.ejmech.2019.111789
CHEMBL4741242 186294 0 None 2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 476 6 1 6 4.4 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(Br)c1 10.1016/j.ejmech.2019.111789
162646518 186329 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 416 6 1 6 3.8 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(F)c1 10.1016/j.ejmech.2019.111789
CHEMBL4741688 186329 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 416 6 1 6 3.8 O=C(Nc1ccc(S(=O)(=O)Oc2cccc([N+](=O)[O-])c2)cc1)c1cccc(F)c1 10.1016/j.ejmech.2019.111789
146015351 26247 21 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 425 7 5 10 -0.3 CNc1ncnc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
5311303 26247 21 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 425 7 5 10 -0.3 CNc1ncnc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
CHEMBL1096400 26247 21 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 425 7 5 10 -0.3 CNc1ncnc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
CHEMBL129841 26247 21 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 425 7 5 10 -0.3 CNc1ncnc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
162656141 187718 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 414 6 2 3 4.4 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)NCc3cccc(Cl)c3)cc2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4758186 187718 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 414 6 2 3 4.4 Cc1cccc(C(=O)Nc2ccc(S(=O)(=O)NCc3cccc(Cl)c3)cc2)c1 10.1016/j.ejmech.2019.111789
10671020 20993 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 445 6 5 10 -0.1 Nc1nc(Cl)nc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
CHEMBL1094760 20993 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 445 6 5 10 -0.1 Nc1nc(Cl)nc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
CHEMBL1199057 20993 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
ChEMBL 445 6 5 10 -0.1 Nc1nc(Cl)nc2c1ncn2[C@H]1C[C@H](OP(=O)(O)O)[C@@H](COP(=O)(O)O)O1 10.1021/jm901691y
162656021 187567 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1cccc(C(=O)Nc2cccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)c2)c1 10.1016/j.ejmech.2019.111789
CHEMBL4756398 187567 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 412 6 1 6 3.9 Cc1cccc(C(=O)Nc2cccc(S(=O)(=O)Oc3cccc([N+](=O)[O-])c3)c2)c1 10.1016/j.ejmech.2019.111789
15747651 108400 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 263 5 3 3 1.9 COc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL298929 108400 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assayAntagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay
ChEMBL 263 5 3 3 1.9 COc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
1713 7308 68 None 3 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
5957 7308 68 None 3 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
91 7308 68 None 3 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
CHEMBL14249 7308 68 None 3 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
DB00171 7308 68 None 3 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
1783 10697 25 None -3 7 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 18974869
8629 10697 25 None -3 7 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 18974869
CHEMBL375951 10697 25 None -3 7 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 18974869
DB01861 10697 25 None -3 7 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 18974869
1782 10696 16 None -2 5 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 18974869
18068 10696 16 None -2 5 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 18974869
CHEMBL439009 10696 16 None -2 5 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 18974869
DB03501 10696 16 None -2 5 Mouse 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 18974869
1713 7308 68 None 3 10 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21773766
5957 7308 68 None 3 10 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21773766
91 7308 68 None 3 10 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21773766
CHEMBL14249 7308 68 None 3 10 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21773766
DB00171 7308 68 None 3 10 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21773766
3187704 7286 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 12 1 8 4.0 COCCn1nnnc1C(c1cc2cc(OC)ccc2[nH]c1=O)N(Cc1ccccc1)CCc1ccccc1 21744154
5518 7286 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 524 12 1 8 4.0 COCCn1nnnc1C(c1cc2cc(OC)ccc2[nH]c1=O)N(Cc1ccccc1)CCc1ccccc1 21744154
3188786 7287 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 535 10 4 9 2.8 COc1ccc(cc1)CNC(=O)C(N(C(=O)c1snc(c1N)C(=O)N)Cc1ccco1)c1ccc(cc1)O 21744154
5519 7287 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 535 10 4 9 2.8 COc1ccc(cc1)CNC(=O)C(N(C(=O)c1snc(c1N)C(=O)N)Cc1ccco1)c1ccc(cc1)O 21744154
CHEMBL1466483 7287 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 535 10 4 9 2.8 COc1ccc(cc1)CNC(=O)C(N(C(=O)c1snc(c1N)C(=O)N)Cc1ccco1)c1ccc(cc1)O 21744154
3354 9148 26 None 2 4 Mouse 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 18974869
5280493 9148 26 None 2 4 Mouse 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 18974869
CHEMBL451509 9148 26 None 2 4 Mouse 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 18974869
DB08855 9148 26 None 2 4 Mouse 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 18974869
3353 9149 0 None 4 4 Mouse 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 18974869
3412 9149 0 None 4 4 Mouse 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 18974869
6435286 9149 0 None 4 4 Mouse 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 18974869
CHEMBL1521056 9149 0 None 4 4 Mouse 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 18974869
3352 9150 28 None 4 4 Mouse 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 18974869
5280879 9150 28 None 4 4 Mouse 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 18974869
5863 9150 28 None 4 4 Mouse 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 18974869
CHEMBL509456 9150 28 None 4 4 Mouse 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 18974869
135439060 7289 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 531 4 2 6 4.6 O=C(N1CCC(CC1)c1nc(=O)c2c([nH]1)n(nn2)Cc1ccccc1Cl)Nc1ccc(cc1)C(F)(F)F 21744154
5524 7289 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 531 4 2 6 4.6 O=C(N1CCC(CC1)c1nc(=O)c2c([nH]1)n(nn2)Cc1ccccc1Cl)Nc1ccc(cc1)C(F)(F)F 21744154
3167869 7285 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 8 1 7 5.1 COc1ccc(cc1)n1c(nnc1c1ccccc1OC)SC(C(=O)Nc1ccccc1)C 21744154
5517 7285 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 8 1 7 5.1 COc1ccc(cc1)n1c(nnc1c1ccccc1OC)SC(C(=O)Nc1ccccc1)C 21744154
3191600 7288 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 517 9 1 7 3.6 COc1ccc(cc1)N(C(c1ccc(cc1)F)C(=O)NCC1CCCO1)C(=O)Cn1nnc2c1cccc2 21744154
5520 7288 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 517 9 1 7 3.6 COc1ccc(cc1)N(C(c1ccc(cc1)F)C(=O)NCC1CCCO1)C(=O)Cn1nnc2c1cccc2 21744154
146015339 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16990797
146015339 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 20148890
1749 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16990797
1749 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 20148890
6031 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16990797
6031 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 20148890
CHEMBL130266 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16990797
CHEMBL130266 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 20148890
DB03435 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16990797
DB03435 10694 32 None -3 7 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 20148890
1782 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 16990797
1782 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 20148890
18068 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 16990797
18068 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 20148890
CHEMBL439009 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 16990797
CHEMBL439009 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 20148890
DB03501 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 16990797
DB03501 10696 16 None -1 5 Human 7.4 pEC50 = 7.4 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 20148890
1783 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 16990797
1783 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 20148890
8629 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 16990797
8629 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 20148890
CHEMBL375951 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 16990797
CHEMBL375951 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 20148890
DB01861 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 16990797
DB01861 10697 25 None 1 7 Human 7.7 pEC50 = 7.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 20148890
3354 9148 26 None -2 4 Human 8.7 pEC50 = 8.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 16990797
5280493 9148 26 None -2 4 Human 8.7 pEC50 = 8.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 16990797
CHEMBL451509 9148 26 None -2 4 Human 8.7 pEC50 = 8.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 16990797
DB08855 9148 26 None -2 4 Human 8.7 pEC50 = 8.7 Functional
[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to 1321N1 cell membranes expressing hGPR17.
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 16990797
3353 9149 0 None -8 4 Human 8.3 pEC50 = 8.3 Functional
[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 16990797
3412 9149 0 None -8 4 Human 8.3 pEC50 = 8.3 Functional
[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 16990797
6435286 9149 0 None -8 4 Human 8.3 pEC50 = 8.3 Functional
[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 16990797
CHEMBL1521056 9149 0 None -8 4 Human 8.3 pEC50 = 8.3 Functional
[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.[<sup>35</sup>S]GTP&gamma;S binding to COS-7 cell membranes expressing hGPR17.
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 16990797
1836 9370 59 None -41 18 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 9370 59 None -41 18 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 9370 59 None -41 18 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 9370 59 None -41 18 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 9370 59 None -41 18 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
1776 7574 38 None -4 4 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O None
5006 7574 38 None -4 4 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O None
9854012 7574 38 None -4 4 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O None
CHEMBL334966 7574 38 None -4 4 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O None
DB06441 7574 38 None -4 4 Mouse 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O None
1836 9370 59 None -41 18 Mouse 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 18974869
3340 9370 59 None -41 18 Mouse 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 18974869
5281040 9370 59 None -41 18 Mouse 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 18974869
CHEMBL787 9370 59 None -41 18 Mouse 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 18974869
DB00471 9370 59 None -41 18 Mouse 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 18974869
1776 7574 38 None -4 4 Mouse 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 18974869
5006 7574 38 None -4 4 Mouse 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 18974869
9854012 7574 38 None -4 4 Mouse 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 18974869
CHEMBL334966 7574 38 None -4 4 Mouse 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 18974869
DB06441 7574 38 None -4 4 Mouse 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 775 15 7 15 2.9 CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O 18974869


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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
446916 112902 72 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve studyBinding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve study
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
CHEMBL31344 112902 72 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve studyBinding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve study
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
CHEMBL3264006 112902 72 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve studyBinding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve study
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
446916 112902 72 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukastDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukast
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
CHEMBL31344 112902 72 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukastDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukast
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
CHEMBL3264006 112902 72 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukastDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukast
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
145971828 171344 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4215280 171344 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 367 10 3 3 4.5 CCCCCCOc1cc(Cl)c2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
145977144 170624 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 333 10 3 3 3.8 CCCCCCOc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
CHEMBL4206497 170624 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 333 10 3 3 3.8 CCCCCCOc1ccc2c(CCC(=O)O)c(C(=O)O)[nH]c2c1 10.1021/acs.jmedchem.7b01768
6450546 179227 24 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 374 4 3 2 4.8 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12)Nc1ccccc1 10.1021/ml400399f
CHEMBL419045 179227 24 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 374 4 3 2 4.8 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12)Nc1ccccc1 10.1021/ml400399f
CHEMBL44793 179227 24 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 374 4 3 2 4.8 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12)Nc1ccccc1 10.1021/ml400399f
446916 112902 72 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
CHEMBL31344 112902 72 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
CHEMBL3264006 112902 72 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assay
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/ml400399f
446916 112902 72 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL31344 112902 72 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
CHEMBL3264006 112902 72 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting
ChEMBL 301 4 3 2 3.2 O=C(O)CCc1c(C(=O)O)[nH]c2cc(Cl)cc(Cl)c12 10.1021/acs.jmedchem.7b01768
2237 9936 79 None -54 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/ml400399f
3634 9936 79 None -54 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/ml400399f
4887 9936 79 None -54 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/ml400399f
CHEMBL21333 9936 79 None -54 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/ml400399f
DB01411 9936 79 None -54 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/ml400399f
1836 9370 59 None -87 15 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/ml400399f
3340 9370 59 None -87 15 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/ml400399f
5281040 9370 59 None -87 15 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/ml400399f
CHEMBL787 9370 59 None -87 15 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/ml400399f
DB00471 9370 59 None -87 15 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/ml400399f
1836 9370 59 None -87 15 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 9370 59 None -87 15 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 9370 59 None -87 15 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 9370 59 None -87 15 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 9370 59 None -87 15 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
2237 9936 79 None -54 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
3634 9936 79 None -54 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
4887 9936 79 None -54 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
CHEMBL21333 9936 79 None -54 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
DB01411 9936 79 None -54 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayDisplacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None