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
| |
| 91826086 | 115000 | None | 44 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 2398 | 4 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342358 | 115000 | None | 44 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 2398 | 4 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 118716417 | 115018 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | 10 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 384 | 7 | 3 | 7 | 2.6 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342376 | 115018 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | 10 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 384 | 7 | 3 | 7 | 2.6 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 118716420 | 115021 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342379 | 115021 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 7803 | 993 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | ||
| 86277841 | 993 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | ||
| CHEMBL3342370 | 993 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | ||
| 118716418 | 115019 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 348 | 6 | 3 | 6 | 3.2 | CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342377 | 115019 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 348 | 6 | 3 | 6 | 3.2 | CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 91826086 | 115000 | None | 44 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2398 | 4 | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342358 | 115000 | None | 44 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2398 | 4 | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 7803 | 993 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | -1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | ||
| 86277841 | 993 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | -1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | ||
| CHEMBL3342370 | 993 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | -1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | ||
| 91826086 | 115000 | None | 44 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2398 | 4 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342358 | 115000 | None | 44 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2398 | 4 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 118716420 | 115021 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342379 | 115021 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 137639471 | 156988 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 4 | 2 | 7 | 2.6 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(F)cc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4072160 | 156988 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 4 | 2 | 7 | 2.6 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(F)cc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| 118716413 | 115013 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 60 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 393 | 6 | 2 | 5 | 4.8 | FC(F)(F)CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342371 | 115013 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 60 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 393 | 6 | 2 | 5 | 4.8 | FC(F)(F)CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 137661197 | 159428 | None | 1 | Human | Functional | pEC50 | = | 8.8 | 8.8 | -3 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4100119 | 159428 | None | 1 | Human | Functional | pEC50 | = | 8.8 | 8.8 | -3 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| 137633277 | 156672 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 388 | 3 | 3 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)Nc1ccccc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4068635 | 156672 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 388 | 3 | 3 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)Nc1ccccc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| 137644326 | 158190 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 5 | 2 | 9 | 1.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1nccc1C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4086570 | 158190 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 5 | 2 | 9 | 1.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1nccc1C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| 118716409 | 115008 | None | 0 | Mouse | Functional | pEC50 | = | 8 | 8.0 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342366 | 115008 | None | 0 | Mouse | Functional | pEC50 | = | 8 | 8.0 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 118716404 | 115003 | None | 0 | Mouse | Functional | pEC50 | = | 5 | 5.0 | -4 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 299 | 8 | 2 | 6 | 2.4 | COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342361 | 115003 | None | 0 | Mouse | Functional | pEC50 | = | 5 | 5.0 | -4 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 299 | 8 | 2 | 6 | 2.4 | COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 118716406 | 115005 | None | 0 | Mouse | Functional | pEC50 | = | 5 | 5.0 | 2 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 226 | 4 | 1 | 4 | 2.4 | c1ccc(-c2cc(NCC3CC3)ncn2)nc1 | 10.1021/ml500240d | ||
| CHEMBL3342363 | 115005 | None | 0 | Mouse | Functional | pEC50 | = | 5 | 5.0 | 2 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 226 | 4 | 1 | 4 | 2.4 | c1ccc(-c2cc(NCC3CC3)ncn2)nc1 | 10.1021/ml500240d | ||
| 118716401 | 114894 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | -3 | 2 | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 510 | 10 | 3 | 7 | 4.4 | O=S(=O)(NC[C@H]1CC[C@H](CNc2cc(-c3ccccn3)nc(NC3CC3)n2)CC1)c1cccc(F)c1 | 10.1021/ml500240d | ||
| CHEMBL3341764 | 114894 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | -3 | 2 | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 510 | 10 | 3 | 7 | 4.4 | O=S(=O)(NC[C@H]1CC[C@H](CNc2cc(-c3ccccn3)nc(NC3CC3)n2)CC1)c1cccc(F)c1 | 10.1021/ml500240d | ||
| 118716409 | 115008 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | -1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342366 | 115008 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | -1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 5407221 | 155994 | None | 8 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 319 | 3 | 3 | 4 | 3.3 | C/C(=N\NC(=O)c1cc2ccccc2cc1O)c1ccc(N)cc1 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4060705 | 155994 | None | 8 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 319 | 3 | 3 | 4 | 3.3 | C/C(=N\NC(=O)c1cc2ccccc2cc1O)c1ccc(N)cc1 | 10.1021/acs.jmedchem.6b00648 | ||
| 137645445 | 157629 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assay |
ChEMBL | 341 | 4 | 2 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(C)C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4080106 | 157629 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assay |
ChEMBL | 341 | 4 | 2 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(C)C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| 118716402 | 115001 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 255 | 5 | 2 | 5 | 2.4 | CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342359 | 115001 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 255 | 5 | 2 | 5 | 2.4 | CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 118716412 | 115011 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 362 | 6 | 2 | 6 | 3.2 | CNc1nc(NCc2ccc(N(C)C(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| CHEMBL3342369 | 115011 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 362 | 6 | 2 | 6 | 3.2 | CNc1nc(NCc2ccc(N(C)C(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | ||
| 137661197 | 159428 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | -3 | 2 | Agonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assayAgonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
| CHEMBL4100119 | 159428 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | -3 | 2 | Agonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assayAgonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | ||
Showing 1 to 50 of 300 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
| |
| 168269293 | 190082 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5170821 | 190082 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
| 76313672 | 103972 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 | 10.1021/ml400275z | ||
| CHEMBL3092410 | 103972 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 | 10.1021/ml400275z | ||
| 168292047 | 192048 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 278 | 4 | 1 | 5 | 3.4 | CNc1nc(Oc2ccccc2)cc(-c2ccccn2)n1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5200611 | 192048 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 278 | 4 | 1 | 5 | 3.4 | CNc1nc(Oc2ccccc2)cc(-c2ccccn2)n1 | 10.1016/j.bmcl.2022.128607 | ||
| 168284637 | 191588 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 331 | 4 | 3 | 4 | 2.6 | NC(Cc1cnc[nH]1)c1nc2ccc(-c3ccccc3)cc2c(=O)[nH]1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5193472 | 191588 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 331 | 4 | 3 | 4 | 2.6 | NC(Cc1cnc[nH]1)c1nc2ccc(-c3ccccc3)cc2c(=O)[nH]1 | 10.1016/j.bmcl.2022.128607 | ||
| 168269293 | 190082 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5170821 | 190082 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
| 76317176 | 103974 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 443 | 9 | 1 | 4 | 4.1 | COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 | 10.1021/ml400275z | ||
| CHEMBL3092412 | 103974 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 443 | 9 | 1 | 4 | 4.1 | COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 | 10.1021/ml400275z | ||
| 76331797 | 103973 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 | 10.1021/ml400275z | ||
| CHEMBL3092411 | 103973 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 | 10.1021/ml400275z | ||
| 168275606 | 190724 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 362 | 6 | 1 | 5 | 2.5 | O=C(Cc1nn(CC2CCC2)c(=O)c2ccccc12)NCc1ccccn1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5180932 | 190724 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 362 | 6 | 1 | 5 | 2.5 | O=C(Cc1nn(CC2CCC2)c(=O)c2ccccc12)NCc1ccccn1 | 10.1016/j.bmcl.2022.128607 | ||
| 124263402 | 191719 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 283 | 4 | 2 | 5 | 3.3 | CNc1cc(-c2ccccn2)nc(NC2CCCCC2)n1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5195424 | 191719 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 283 | 4 | 2 | 5 | 3.3 | CNc1cc(-c2ccccn2)nc(NC2CCCCC2)n1 | 10.1016/j.bmcl.2022.128607 | ||
| 73211886 | 1017 | None | 3 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 352 | 3 | 0 | 6 | 2.6 | N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl | 10.1021/ml400275z | ||
| 7800 | 1017 | None | 3 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 352 | 3 | 0 | 6 | 2.6 | N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl | 10.1021/ml400275z | ||
| CHEMBL3092413 | 1017 | None | 3 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 352 | 3 | 0 | 6 | 2.6 | N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl | 10.1021/ml400275z | ||
| 168292856 | 192217 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 389 | 7 | 2 | 6 | 2.9 | Cn1cc(-c2ccc3nc(C(N)CCOCc4ccccc4)[nH]c(=O)c3c2)cn1 | 10.1016/j.bmcl.2022.128607 | ||
| CHEMBL5203229 | 192217 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 389 | 7 | 2 | 6 | 2.9 | Cn1cc(-c2ccc3nc(C(N)CCOCc4ccccc4)[nH]c(=O)c3c2)cn1 | 10.1016/j.bmcl.2022.128607 | ||
Showing 1 to 23 of 23 entries