Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
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 DOI
11433866 14232 None 2 Human Functional pEC50 = 10.4 10.4 - 1
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 14232 None 2 Human Functional pEC50 = 10.4 10.4 - 1
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 14232 None 2 Human Functional pEC50 = 10.4 10.4 - 1
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 14230 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 14230 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 14230 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 14234 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 14234 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 14234 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 163655 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 163655 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 14246 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 14246 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 14246 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 106181 None 49 Mouse Functional pEC50 = 6.0 6.0 -9 3
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 106181 None 49 Mouse Functional pEC50 = 6.0 6.0 -9 3
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 106181 None 49 Mouse Functional pEC50 = 6.0 6.0 -9 3
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 3922 None 21 Human Functional pEC50 = 5.9 5.9 -3 7
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 3922 None 21 Human Functional pEC50 = 5.9 5.9 -3 7
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 3922 None 21 Human Functional pEC50 = 5.9 5.9 -3 7
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 3922 None 21 Human Functional pEC50 = 5.9 5.9 -3 7
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 3922 None 21 Human Functional pEC50 = 5.9 5.9 -3 7
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 163940 None 0 Human Functional pEC50 = 6.9 6.9 45 2
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 163940 None 0 Human Functional pEC50 = 6.9 6.9 45 2
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 164157 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164157 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 106068 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 106068 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 143441 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 143441 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 164908 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 164908 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 164696 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 164696 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 143441 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 143441 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 194929 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 194929 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 217551 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 164187 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 164187 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 106070 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 106070 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 217551 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 146446 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 146446 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 217365 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 106068 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 106068 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 101249 None 4 Human Functional pEC50 = 7.7 7.7 - 1
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 101249 None 4 Human Functional pEC50 = 7.7 7.7 - 1
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 106068 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 106068 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 106073 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 106073 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 164660 None 0 Rat Functional pEC50 = 5.6 5.6 -33 3
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 164660 None 0 Rat Functional pEC50 = 5.6 5.6 -33 3
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 217551 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 217551 None 0 Human Functional pEC50 = 4.6 4.6 - 1
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 164759 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 164759 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 189028 None 7 Human Functional pEC50 = 6.6 6.6 - 1
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 189028 None 7 Human Functional pEC50 = 6.6 6.6 - 1
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 188493 None 4 Human Functional pEC50 = 4.5 4.5 - 1
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 188493 None 4 Human Functional pEC50 = 4.5 4.5 - 1
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 163921 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 163921 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 145649 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 145649 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 145649 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 145649 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 164660 None 0 Mouse Functional pEC50 = 5.5 5.5 -44 3
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 164660 None 0 Mouse Functional pEC50 = 5.5 5.5 -44 3
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 106073 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 106073 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 106073 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 106073 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 163846 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 163846 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 106181 None 49 Human Functional pEC50 = 6.5 6.5 5 3
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 106181 None 49 Human Functional pEC50 = 6.5 6.5 5 3
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 106181 None 49 Human Functional pEC50 = 6.5 6.5 5 3
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 143441 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 143441 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164297 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164297 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 106074 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 106074 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 101249 None 4 Human Functional pEC50 = 5.4 5.4 - 1
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 101249 None 4 Human Functional pEC50 = 5.4 5.4 - 1
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 101249 None 4 Human Functional pEC50 = 5.4 5.4 - 1
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 101249 None 4 Human Functional pEC50 = 5.4 5.4 - 1
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 163787 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 163787 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 145649 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 145649 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164205 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 164205 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 217365 None 0 Human Functional pEC50 = 4.4 4.4 - 1
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 164345 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 164345 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 106072 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 106072 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 106069 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 106069 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 106069 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 106069 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 106069 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 106069 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 164371 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 164371 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 164939 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 164939 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 106071 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 106071 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 146446 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 146446 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 163940 None 0 Rat Functional pEC50 = 5.3 5.3 -45 2
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 163940 None 0 Rat Functional pEC50 = 5.3 5.3 -45 2
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 146446 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 146446 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 217365 None 0 Human Functional pEC50 = 4.2 4.2 - 1
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 106181 None 49 Human Functional pEC50 = 8.2 8.2 5 3
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 106181 None 49 Human Functional pEC50 = 8.2 8.2 5 3
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 106181 None 49 Human Functional pEC50 = 8.2 8.2 5 3
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 164794 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 164794 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 164660 None 0 Human Functional pEC50 = 7.2 7.2 33 3
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 164660 None 0 Human Functional pEC50 = 7.2 7.2 33 3
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 106181 None 49 Rat Functional pEC50 = 6.2 6.2 -5 3
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 106181 None 49 Rat Functional pEC50 = 6.2 6.2 -5 3
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 106181 None 49 Rat Functional pEC50 = 6.2 6.2 -5 3
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 106075 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 106075 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 106075 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 106075 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 106075 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 106075 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 152291 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 152291 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 152291 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 152291 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 152291 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 152291 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 194929 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 194929 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 194929 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 194929 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 217365 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 163915 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 163915 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 106181 None 49 Human Functional pEC50 = 6.1 6.1 5 3
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 106181 None 49 Human Functional pEC50 = 6.1 6.1 5 3
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 106181 None 49 Human Functional pEC50 = 6.1 6.1 5 3
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 201770 None 0 Human Functional pEC50 = 6.0 6.0 -43 2
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 201770 None 0 Human Functional pEC50 = 6.0 6.0 -43 2
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 201770 None 0 Human Functional pEC50 = 6.0 6.0 -43 2
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 201770 None 0 Human Functional pEC50 = 6.0 6.0 -43 2
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 164870 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 164870 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 787 None 27 Human Functional pIC50 = 9.2 9.2 2 4
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 787 None 27 Human Functional pIC50 = 9.2 9.2 2 4
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 787 None 27 Human Functional pIC50 = 9.2 9.2 2 4
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
9854012.0 787 None 27 Human Functional pIC50 = 9.2 9.2 2 4
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 787 None 27 Human Functional pIC50 = 9.2 9.2 2 4
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 787 None 27 Human Functional pIC50 = 9.2 9.2 2 4
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 14225 None 5 Human Functional pIC50 = 7.0 7.0 169 2
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 14225 None 5 Human Functional pIC50 = 7.0 7.0 169 2
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 14225 None 5 Human Functional pIC50 = 7.0 7.0 169 2
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 180190 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 180190 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 180530 None 0 Human Functional pIC50 = 5.8 5.8 9 2
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 180530 None 0 Human Functional pIC50 = 5.8 5.8 9 2
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 180220 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 180220 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 179783 None 10 Human Functional pIC50 = 5.8 5.8 3 2
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 179783 None 10 Human Functional pIC50 = 5.8 5.8 3 2
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 182143 None 0 Human Functional pIC50 = 5.7 5.7 1 3
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 182143 None 0 Human Functional pIC50 = 5.7 5.7 1 3
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 181855 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 181855 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 2027 None 69 Human Functional pIC50 = 4.5 4.5 -74 7
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 179764 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
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 179764 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
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 180397 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 180397 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 183394 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 183394 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 182393 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 182393 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 180657 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
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 180657 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
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 183409 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 183409 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 181616 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 181616 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 183587 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 183587 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 179621 None 0 Human Functional pIC50 = 5.4 5.4 2 2
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 179621 None 0 Human Functional pIC50 = 5.4 5.4 2 2
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 179656 None 0 Human Functional pIC50 = 5.3 5.3 1 2
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 179656 None 0 Human Functional pIC50 = 5.3 5.3 1 2
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 19482 None 17 Human Functional pIC50 = 6.3 6.3 -1 3
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 19482 None 17 Human Functional pIC50 = 6.3 6.3 -1 3
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 19482 None 17 Human Functional pIC50 = 6.3 6.3 -1 3
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 19482 None 17 Human Functional pIC50 = 6.3 6.3 -1 3
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 181045 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 181045 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 14226 None 0 Human Functional pIC50 = 6.2 6.2 1 2
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 14226 None 0 Human Functional pIC50 = 6.2 6.2 1 2
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 14226 None 0 Human Functional pIC50 = 6.2 6.2 1 2
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 180894 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 180894 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 101678 None 2 Human Functional pIC50 = 5.1 5.1 - 1
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 101678 None 2 Human Functional pIC50 = 5.1 5.1 - 1
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 520 None 42 Human Functional pEC50 = 8.1 8.1 3 10
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 520 None 42 Human Functional pEC50 = 8.1 8.1 3 10
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
91 520 None 42 Human Functional pEC50 = 8.1 8.1 3 10
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 520 None 42 Human Functional pEC50 = 8.1 8.1 3 10
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 520 None 42 Human Functional pEC50 = 8.1 8.1 3 10
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 3925 None 23 Mouse Functional pEC50 = 7.2 7.2 -3 7
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 3925 None 23 Mouse Functional pEC50 = 7.2 7.2 -3 7
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 3925 None 23 Mouse Functional pEC50 = 7.2 7.2 -3 7
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 3925 None 23 Mouse Functional pEC50 = 7.2 7.2 -3 7
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 3924 None 14 Mouse Functional pEC50 = 7.2 7.2 -2 5
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 3924 None 14 Mouse Functional pEC50 = 7.2 7.2 -2 5
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 3924 None 14 Mouse Functional pEC50 = 7.2 7.2 -2 5
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 3924 None 14 Mouse Functional pEC50 = 7.2 7.2 -2 5
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 520 None 42 Human Functional pEC50 = 7.4 7.4 3 10
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 520 None 42 Human Functional pEC50 = 7.4 7.4 3 10
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
91 520 None 42 Human Functional pEC50 = 7.4 7.4 3 10
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 520 None 42 Human Functional pEC50 = 7.4 7.4 3 10
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 520 None 42 Human Functional pEC50 = 7.4 7.4 3 10
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 498 None 0 Human Functional pEC50 = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 524 12 1 8 4.0 COCCn1nnnc1C(c1cc2cc(OC)ccc2[nH]c1=O)N(Cc1ccccc1)CCc1ccccc1 21744154
5518 498 None 0 Human Functional pEC50 = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 524 12 1 8 4.0 COCCn1nnnc1C(c1cc2cc(OC)ccc2[nH]c1=O)N(Cc1ccccc1)CCc1ccccc1 21744154
3188786 499 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 499 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 499 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 2369 None 23 Mouse Functional pEC50 = 9.1 9.1 2 4
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 2369 None 23 Mouse Functional pEC50 = 9.1 9.1 2 4
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 2369 None 23 Mouse Functional pEC50 = 9.1 9.1 2 4
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 2369 None 23 Mouse Functional pEC50 = 9.1 9.1 2 4
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 2370 None 0 Mouse Functional pEC50 = 9.2 9.2 4 4
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 2370 None 0 Mouse Functional pEC50 = 9.2 9.2 4 4
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 2370 None 0 Mouse Functional pEC50 = 9.2 9.2 4 4
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 2370 None 0 Mouse Functional pEC50 = 9.2 9.2 4 4
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 2371 None 24 Mouse Functional pEC50 = 9.5 9.5 4 4
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 2371 None 24 Mouse Functional pEC50 = 9.5 9.5 4 4
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 2371 None 24 Mouse Functional pEC50 = 9.5 9.5 4 4
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 2371 None 24 Mouse Functional pEC50 = 9.5 9.5 4 4
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 501 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 501 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 497 None 0 Human Functional pEC50 = 10.0 10.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 460 8 1 7 5.1 COc1ccc(cc1)n1c(nnc1c1ccccc1OC)SC(C(=O)Nc1ccccc1)C 21744154
5517 497 None 0 Human Functional pEC50 = 10.0 10.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 460 8 1 7 5.1 COc1ccc(cc1)n1c(nnc1c1ccccc1OC)SC(C(=O)Nc1ccccc1)C 21744154
3191600 500 None 0 Human Functional pEC50 = 10.0 10.0 - 1
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 500 None 0 Human Functional pEC50 = 10.0 10.0 - 1
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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3922 None 21 Human Functional pEC50 = 7.4 7.4 -3 7
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3924 None 14 Human Functional pEC50 = 7.4 7.4 -1 5
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 3925 None 23 Human Functional pEC50 = 7.7 7.7 1 7
[<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 2369 None 23 Human Functional pEC50 = 8.7 8.7 -2 4
[<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 2369 None 23 Human Functional pEC50 = 8.7 8.7 -2 4
[<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 2369 None 23 Human Functional pEC50 = 8.7 8.7 -2 4
[<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 2369 None 23 Human Functional pEC50 = 8.7 8.7 -2 4
[<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 2370 None 0 Human Functional pEC50 = 8.3 8.3 -8 4
[<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 2370 None 0 Human Functional pEC50 = 8.3 8.3 -8 4
[<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 2370 None 0 Human Functional pEC50 = 8.3 8.3 -8 4
[<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 2370 None 0 Human Functional pEC50 = 8.3 8.3 -8 4
[<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 2592 None 44 Mouse Functional pIC50 = 8.1 8.1 -41 20
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 2592 None 44 Mouse Functional pIC50 = 8.1 8.1 -41 20
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 2592 None 44 Mouse Functional pIC50 = 8.1 8.1 -41 20
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
5281040.0 2592 None 44 Mouse Functional pIC50 = 8.1 8.1 -41 20
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 2592 None 44 Mouse Functional pIC50 = 8.1 8.1 -41 20
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 2592 None 44 Mouse Functional pIC50 = 8.1 8.1 -41 20
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 787 None 27 Mouse Functional pIC50 = 8.1 8.1 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.1 8.1 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.1 8.1 -4 4
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
9854012.0 787 None 27 Mouse Functional pIC50 = 8.1 8.1 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.1 8.1 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.1 8.1 -4 4
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 2592 None 44 Mouse Functional pIC50 = 7.2 7.2 -41 20
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 2592 None 44 Mouse Functional pIC50 = 7.2 7.2 -41 20
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 2592 None 44 Mouse Functional pIC50 = 7.2 7.2 -41 20
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
5281040.0 2592 None 44 Mouse Functional pIC50 = 7.2 7.2 -41 20
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 2592 None 44 Mouse Functional pIC50 = 7.2 7.2 -41 20
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 2592 None 44 Mouse Functional pIC50 = 7.2 7.2 -41 20
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 787 None 27 Mouse Functional pIC50 = 8.9 8.9 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.9 8.9 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.9 8.9 -4 4
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
9854012.0 787 None 27 Mouse Functional pIC50 = 8.9 8.9 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.9 8.9 -4 4
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 787 None 27 Mouse Functional pIC50 = 8.9 8.9 -4 4
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 (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
446916 106181 None 49 Human Binding pKd = 5.9 5.9 - 1
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 106181 None 49 Human Binding pKd = 5.9 5.9 - 1
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 106181 None 49 Human Binding pKd = 5.9 5.9 - 1
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 106181 None 49 Human Binding pKi = 5.9 5.9 - 1
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 106181 None 49 Human Binding pKi = 5.9 5.9 - 1
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 106181 None 49 Human Binding pKi = 5.9 5.9 - 1
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 164660 None 0 Human Binding pKi = 4.9 4.9 - 1
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 164660 None 0 Human Binding pKi = 4.9 4.9 - 1
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 163940 None 0 Human Binding pKi = 5.8 5.8 - 1
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 163940 None 0 Human Binding pKi = 5.8 5.8 - 1
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 172551 None 21 Human Binding pKi = 5.8 5.8 - 1
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 172551 None 21 Human Binding pKi = 5.8 5.8 - 1
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 172551 None 21 Human Binding pKi = 5.8 5.8 - 1
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 106181 None 49 Human Binding pKi = 5.6 5.6 - 1
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 106181 None 49 Human Binding pKi = 5.6 5.6 - 1
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 106181 None 49 Human Binding pKi = 5.6 5.6 - 1
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 106181 None 49 Human Binding pKi = 5.6 5.6 - 1
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 106181 None 49 Human Binding pKi = 5.6 5.6 - 1
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 106181 None 49 Human Binding pKi = 5.6 5.6 - 1
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 3162 None 53 Human Binding pKi = 5.4 5.4 -54 3
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 3162 None 53 Human Binding pKi = 5.4 5.4 -54 3
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 3162 None 53 Human Binding pKi = 5.4 5.4 -54 3
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
4887.0 3162 None 53 Human Binding pKi = 5.4 5.4 -54 3
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 3162 None 53 Human Binding pKi = 5.4 5.4 -54 3
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 3162 None 53 Human Binding pKi = 5.4 5.4 -54 3
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 2592 None 44 Human Binding pKi = 5.2 5.2 -87 15
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 2592 None 44 Human Binding pKi = 5.2 5.2 -87 15
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 2592 None 44 Human Binding pKi = 5.2 5.2 -87 15
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
5281040.0 2592 None 44 Human Binding pKi = 5.2 5.2 -87 15
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 2592 None 44 Human Binding pKi = 5.2 5.2 -87 15
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 2592 None 44 Human Binding pKi = 5.2 5.2 -87 15
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 2592 None 44 Human Binding pKi = 8.3 8.3 -87 15
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 2592 None 44 Human Binding pKi = 8.3 8.3 -87 15
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 2592 None 44 Human Binding pKi = 8.3 8.3 -87 15
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
5281040.0 2592 None 44 Human Binding pKi = 8.3 8.3 -87 15
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 2592 None 44 Human Binding pKi = 8.3 8.3 -87 15
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 2592 None 44 Human Binding pKi = 8.3 8.3 -87 15
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 3162 None 53 Human Binding pKi = 8.3 8.3 -54 3
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 3162 None 53 Human Binding pKi = 8.3 8.3 -54 3
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 3162 None 53 Human Binding pKi = 8.3 8.3 -54 3
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
4887.0 3162 None 53 Human Binding pKi = 8.3 8.3 -54 3
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 3162 None 53 Human Binding pKi = 8.3 8.3 -54 3
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 3162 None 53 Human Binding pKi = 8.3 8.3 -54 3
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