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 14112 3 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 14112 3 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 14112 3 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 14110 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 14110 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 14110 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 14114 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 14114 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 14114 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 163008 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 163008 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 14126 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 14126 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 14126 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 105645 65 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 105645 65 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 105645 65 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 163293 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 163293 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 163510 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 163510 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 105532 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 105532 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 142822 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 142822 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 164261 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 164261 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 164049 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 164049 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 142822 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 142822 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 193149 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 193149 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 213288 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 163540 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 163540 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 105534 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 105534 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 213288 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 145825 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 145825 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 213104 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 105532 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 105532 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 100725 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 100725 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 105532 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 105532 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 105537 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 105537 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 164013 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 164013 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 213288 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 213288 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 164112 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 164112 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 188333 4 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 188333 4 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 187802 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 187802 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 163274 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 163274 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 145028 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 145028 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 145028 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 145028 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 164013 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 164013 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 105537 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 105537 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 105537 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 105537 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 163199 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 163199 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 105645 65 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 105645 65 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 105645 65 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 142822 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 142822 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 163650 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 163650 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 105538 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 105538 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 100725 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 100725 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 100725 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 100725 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 163140 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 163140 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 145028 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 145028 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 163558 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 163558 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 213104 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 163698 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 163698 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 105536 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 105536 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 105533 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 105533 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 105533 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 105533 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 105533 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 105533 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 163724 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 163724 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 164292 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 164292 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 105535 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 105535 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 145825 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 145825 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 163293 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 163293 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 145825 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 145825 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 213104 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 105645 65 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 105645 65 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 105645 65 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 164147 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 164147 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 164013 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 164013 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 105645 65 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 105645 65 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 105645 65 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 105539 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 105539 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 105539 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 105539 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 105539 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 105539 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 151670 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 151670 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 151670 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 151670 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 151670 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 151670 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 193149 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 193149 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 193149 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 193149 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 213104 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 163268 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 163268 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 105645 65 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 105645 65 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 105645 65 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 197634 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 197634 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 197634 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 197634 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 164223 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 164223 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 775 34 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 775 34 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 775 34 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 775 34 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 775 34 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 14105 3 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 14105 3 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 14105 3 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 179504 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 179504 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 179843 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 179843 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 179534 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 179534 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 179097 4 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 179097 4 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 181455 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 181455 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 181167 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 181167 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 1996 116 None -74 3 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 179078 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 179078 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 179711 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 179711 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 182706 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 182706 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 181705 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 181705 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 179969 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 179969 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 182721 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 182721 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 180928 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 180928 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 182899 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 182899 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 178935 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 178935 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 178970 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 178970 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 19275 15 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 19275 15 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 19275 15 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 19275 15 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 180357 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 180357 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 14106 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 14106 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 14106 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 180206 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 180206 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 101152 1 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 101152 1 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 516 63 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 516 63 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
91 516 63 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 516 63 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 516 63 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 3862 18 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 3862 18 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 3862 18 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 3862 18 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 3861 13 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 3861 13 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 3861 13 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 3861 13 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 516 63 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 516 63 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
91 516 63 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 516 63 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 516 63 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 495 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 495 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 496 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 496 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 496 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 2337 24 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 2337 24 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 2337 24 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 2337 24 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 2338 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 2338 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 2338 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 2338 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 2339 25 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 2339 25 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 2339 25 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 2339 25 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 498 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 498 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 494 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 494 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 497 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 497 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3859 30 None -2 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 3861 13 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 3861 13 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 3861 13 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 3861 13 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 3861 13 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 3861 13 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 3861 13 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 3861 13 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 3862 18 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 3862 18 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 3862 18 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 3862 18 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 3862 18 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 3862 18 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 3862 18 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 3862 18 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 2337 24 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 2337 24 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 2337 24 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 2337 24 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 2338 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 2338 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 2338 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 2338 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 2554 56 None -41 15 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 2554 56 None -41 15 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 2554 56 None -41 15 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 2554 56 None -41 15 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 2554 56 None -41 15 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 775 34 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 775 34 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 775 34 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 775 34 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 775 34 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 2554 56 None -41 15 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 2554 56 None -41 15 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 2554 56 None -41 15 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 2554 56 None -41 15 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 2554 56 None -41 15 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 775 34 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 775 34 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 775 34 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 775 34 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 775 34 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 105645 65 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 105645 65 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 105645 65 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 105645 65 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 105645 65 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 105645 65 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 164013 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 164013 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 163293 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 163293 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 171882 18 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 171882 18 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 171882 18 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 105645 65 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 105645 65 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 105645 65 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 105645 65 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 105645 65 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 105645 65 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 3113 73 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 3113 73 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 3113 73 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 3113 73 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 3113 73 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 2554 56 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 3113 73 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 3113 73 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 3113 73 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 3113 73 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 3113 73 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