Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 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 | ||
Showing 1 to 50 of 323 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 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 | ||
Showing 1 to 43 of 43 entries