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

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weight		 Rot
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 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
73211886 1017 None 3 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
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 Functional pEC50 = 4.9 4.9 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
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 Functional pEC50 = 4.9 4.9 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
ChEMBL 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 10.1021/ml400275z
137636773 155919 None 0 Human Functional pEC50 = 5.9 5.9 - 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 420 4 3 7 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4059978 155919 None 0 Human Functional pEC50 = 5.9 5.9 - 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 420 4 3 7 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137639471 156988 None 0 Human Functional pEC50 = 6.9 6.9 - 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 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 = 6.9 6.9 - 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 393 4 2 7 2.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137658295 159813 None 0 Human Functional pEC50 = 6.9 6.9 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1C#N)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4104470 159813 None 0 Human Functional pEC50 = 6.9 6.9 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1C#N)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716415 115016 None 0 Human Functional pEC50 = 7.9 7.9 -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 375 6 2 6 4.1 CNc1nc(NCc2ccc(OC(F)(F)F)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342374 115016 None 0 Human Functional pEC50 = 7.9 7.9 -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 375 6 2 6 4.1 CNc1nc(NCc2ccc(OC(F)(F)F)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
118716410 115009 None 0 Human Functional pEC50 = 7.8 7.8 -5 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 325 5 2 5 3.8 CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342367 115009 None 0 Human Functional pEC50 = 7.8 7.8 -5 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 325 5 2 5 3.8 CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
91826086 115000 None 44 Human Functional pEC50 = 7.8 7.8 2398 4
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 418 7 3 7 3.2 CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
CHEMBL3342358 115000 None 44 Human Functional pEC50 = 7.8 7.8 2398 4
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 418 7 3 7 3.2 CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
168280852 190847 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 333 4 1 5 3.9 Cc1cc(NCc2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5182651 190847 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 333 4 1 5 3.9 Cc1cc(NCc2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
118716403 115002 None 0 Mouse Functional pEC50 = 5.8 5.8 3 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 311 6 2 5 3.8 CC(C)(C)CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342360 115002 None 0 Mouse Functional pEC50 = 5.8 5.8 3 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 311 6 2 5 3.8 CC(C)(C)CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
137636882 156159 None 0 Human Functional pEC50 = 6.8 6.8 - 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 388 3 3 7 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4062704 156159 None 0 Human Functional pEC50 = 6.8 6.8 - 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 388 3 3 7 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137649835 157520 None 0 Human Functional pEC50 = 7.8 7.8 - 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 407 5 2 9 1.8 Cc1cc(C)n(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)n1 10.1021/acs.jmedchem.6b00648
CHEMBL4078723 157520 None 0 Human Functional pEC50 = 7.8 7.8 - 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 407 5 2 9 1.8 Cc1cc(C)n(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)n1 10.1021/acs.jmedchem.6b00648
137656189 159127 None 0 Human Functional pEC50 = 7.8 7.8 - 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 379 5 2 9 1.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1cccn1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4096749 159127 None 0 Human Functional pEC50 = 7.8 7.8 - 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 379 5 2 9 1.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1cccn1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
168292509 191750 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 283 4 2 5 3.3 CNc1nc(NC2CCCCC2)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
CHEMBL5195894 191750 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 283 4 2 5 3.3 CNc1nc(NC2CCCCC2)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
137644326 158190 None 0 Human Functional pEC50 = 5.8 5.8 - 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 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 = 5.8 5.8 - 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 393 5 2 9 1.5 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1nccc1C)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716402 115001 None 0 Human Functional pEC50 = 6.8 6.8 -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 255 5 2 5 2.4 CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342359 115001 None 0 Human Functional pEC50 = 6.8 6.8 -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 255 5 2 5 2.4 CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
137648315 157714 None 0 Human Functional pEC50 = 5.8 5.8 - 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 417 5 2 7 3.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4081167 157714 None 0 Human Functional pEC50 = 5.8 5.8 - 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 417 5 2 7 3.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
135634901 157448 None 33 Human Functional pEC50 = 7.8 7.8 -1 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4077818 157448 None 33 Human Functional pEC50 = 7.8 7.8 -1 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
168272604 190492 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 347 4 1 5 4.4 Cc1cc(NC(C)c2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5177479 190492 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 347 4 1 5 4.4 Cc1cc(NC(C)c2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
168287379 191539 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 355 3 0 5 4.4 Cc1cc(N2CCCC2c2ccccc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5192920 191539 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 355 3 0 5 4.4 Cc1cc(N2CCCC2c2ccccc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
3395869 115014 None 0 Mouse Functional pEC50 = 7.8 7.8 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 310 4 1 4 4.1 Cc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342372 115014 None 0 Mouse Functional pEC50 = 7.8 7.8 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 310 4 1 4 4.1 Cc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
135634945 158797 None 6 Human Functional pEC50 = 7.8 7.8 1 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 403 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(OC(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4093273 158797 None 6 Human Functional pEC50 = 7.8 7.8 1 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 403 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(OC(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137661496 159588 None 0 Human Functional pEC50 = 7.8 7.8 - 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 409 3 2 9 1.4 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1nccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4101801 159588 None 0 Human Functional pEC50 = 7.8 7.8 - 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 409 3 2 9 1.4 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1nccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
135634901 157448 None 33 Mouse Functional pEC50 = 6.8 6.8 1 2
Agonist activity at mouse 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 mouse 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4077818 157448 None 33 Mouse Functional pEC50 = 6.8 6.8 1 2
Agonist activity at mouse 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 mouse 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716416 115017 None 0 Mouse Functional pEC50 = 6.7 6.7 -5 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 369 6 2 7 2.6 CNc1nc(NCc2ccc(S(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342375 115017 None 0 Mouse Functional pEC50 = 6.7 6.7 -5 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 369 6 2 7 2.6 CNc1nc(NCc2ccc(S(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
137648191 157930 None 0 Human Functional pEC50 = 8.7 8.7 - 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 409 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4083614 157930 None 0 Human Functional pEC50 = 8.7 8.7 - 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 409 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137643474 158393 None 0 Human Functional pEC50 = 8.7 8.7 - 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 419 6 2 8 2.5 COc1ccc(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)cc1 10.1021/acs.jmedchem.6b00648
CHEMBL4089047 158393 None 0 Human Functional pEC50 = 8.7 8.7 - 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 419 6 2 8 2.5 COc1ccc(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)cc1 10.1021/acs.jmedchem.6b00648
137657224 159797 None 0 Human Functional pEC50 = 8.7 8.7 - 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 353 3 2 7 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC1CCCC1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4104345 159797 None 0 Human Functional pEC50 = 8.7 8.7 - 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 353 3 2 7 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC1CCCC1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716418 115019 None 0 Mouse Functional pEC50 = 8.7 8.7 -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 348 6 3 6 3.2 CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342377 115019 None 0 Mouse Functional pEC50 = 8.7 8.7 -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 348 6 3 6 3.2 CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
137661197 159428 None 1 Mouse Functional pEC50 = 8.6 8.6 3 2
Agonist activity at mouse 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 mouse 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 Mouse Functional pEC50 = 8.6 8.6 3 2
Agonist activity at mouse 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 mouse 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
3722317 158813 None 10 Human Functional pEC50 = 6.7 6.7 - 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 378 6 2 6 2.9 O=C1/C(=C/NCCCO)C(c2ccccc2)=NN1c1nc2ccccc2s1 10.1021/acs.jmedchem.6b00648
CHEMBL4093427 158813 None 10 Human Functional pEC50 = 6.7 6.7 - 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 378 6 2 6 2.9 O=C1/C(=C/NCCCO)C(c2ccccc2)=NN1c1nc2ccccc2s1 10.1021/acs.jmedchem.6b00648
137649835 157520 None 0 Human Functional pEC50 = 5.7 5.7 - 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 407 5 2 9 1.8 Cc1cc(C)n(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)n1 10.1021/acs.jmedchem.6b00648
CHEMBL4078723 157520 None 0 Human Functional pEC50 = 5.7 5.7 - 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 407 5 2 9 1.8 Cc1cc(C)n(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)n1 10.1021/acs.jmedchem.6b00648
118716400 114999 None 0 Human Functional pEC50 = 6.7 6.7 -50 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](CNc2nc(NC3CC3)cc(-c3ccccn3)n2)CC1)c1cccc(F)c1 10.1021/ml500240d
CHEMBL3342357 114999 None 0 Human Functional pEC50 = 6.7 6.7 -50 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](CNc2nc(NC3CC3)cc(-c3ccccn3)n2)CC1)c1cccc(F)c1 10.1021/ml500240d
118716405 115004 None 0 Mouse Functional pEC50 = 7.7 7.7 27 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 415 8 2 6 4.9 FC(F)(F)Oc1ccc(CNc2nc(NCC3CC3)cc(-c3ccccn3)n2)cc1 10.1021/ml500240d
CHEMBL3342362 115004 None 0 Mouse Functional pEC50 = 7.7 7.7 27 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 415 8 2 6 4.9 FC(F)(F)Oc1ccc(CNc2nc(NCC3CC3)cc(-c3ccccn3)n2)cc1 10.1021/ml500240d
118716406 115005 None 0 Human Functional pEC50 = 4.7 4.7 -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 226 4 1 4 2.4 c1ccc(-c2cc(NCC3CC3)ncn2)nc1 10.1021/ml500240d
CHEMBL3342363 115005 None 0 Human Functional pEC50 = 4.7 4.7 -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 226 4 1 4 2.4 c1ccc(-c2cc(NCC3CC3)ncn2)nc1 10.1021/ml500240d
118716404 115003 None 0 Human Functional pEC50 = 5.7 5.7 4 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 299 8 2 6 2.4 COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342361 115003 None 0 Human Functional pEC50 = 5.7 5.7 4 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 299 8 2 6 2.4 COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
137656189 159127 None 0 Human Functional pEC50 = 5.6 5.6 - 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 379 5 2 9 1.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1cccn1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4096749 159127 None 0 Human Functional pEC50 = 5.6 5.6 - 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 379 5 2 9 1.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1cccn1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
135411687 156746 None 7 Human Functional pEC50 = 6.6 6.6 - 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 302 3 4 5 1.9 CC(C)(C)c1cc(C(=O)N/N=C/c2ccc(O)cc2O)[nH]n1 10.1021/acs.jmedchem.6b00648
CHEMBL4069386 156746 None 7 Human Functional pEC50 = 6.6 6.6 - 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 302 3 4 5 1.9 CC(C)(C)c1cc(C(=O)N/N=C/c2ccc(O)cc2O)[nH]n1 10.1021/acs.jmedchem.6b00648
168276005 190740 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 356 3 0 6 3.8 Cc1cc(N2CCCC2c2cccnc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5181167 190740 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 356 3 0 6 3.8 Cc1cc(N2CCCC2c2cccnc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
137654391 158619 None 0 Human Functional pEC50 = 6.6 6.6 - 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 443 4 2 7 3.8 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(Cl)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4091396 158619 None 0 Human Functional pEC50 = 6.6 6.6 - 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 443 4 2 7 3.8 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(Cl)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137638361 156928 None 0 Human Functional pEC50 = 6.6 6.6 - 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 408 4 3 8 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1cccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4071347 156928 None 0 Human Functional pEC50 = 6.6 6.6 - 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 408 4 3 8 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1cccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137635316 156229 None 0 Human Functional pEC50 = 6.6 6.6 - 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 407 3 2 8 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4063554 156229 None 0 Human Functional pEC50 = 6.6 6.6 - 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 407 3 2 8 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716414 115015 None 0 Human Functional pEC50 = 7.6 7.6 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 365 5 2 5 4.7 CNc1nc(NC2(c3ccc(Cl)cc3)CCC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342373 115015 None 0 Human Functional pEC50 = 7.6 7.6 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 365 5 2 5 4.7 CNc1nc(NC2(c3ccc(Cl)cc3)CCC2)cc(-c2ccccn2)n1 10.1021/ml500240d
168272604 190492 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 347 4 1 5 4.4 Cc1cc(NC(C)c2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5177479 190492 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 347 4 1 5 4.4 Cc1cc(NC(C)c2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
118716412 115011 None 0 Mouse Functional pEC50 = 5.6 5.6 -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 362 6 2 6 3.2 CNc1nc(NCc2ccc(N(C)C(C)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342369 115011 None 0 Mouse Functional pEC50 = 5.6 5.6 -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 362 6 2 6 3.2 CNc1nc(NCc2ccc(N(C)C(C)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
135634945 158797 None 6 Human Functional pEC50 = 5.6 5.6 1 2
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 403 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(OC(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4093273 158797 None 6 Human Functional pEC50 = 5.6 5.6 1 2
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 403 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(OC(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
135634901 157448 None 33 Human Functional pEC50 = 6.6 6.6 -1 2
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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4077818 157448 None 33 Human Functional pEC50 = 6.6 6.6 -1 2
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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137647882 157795 None 0 Human Functional pEC50 = 5.5 5.5 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4081885 157795 None 0 Human Functional pEC50 = 5.5 5.5 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716417 115018 None 0 Human Functional pEC50 = 8.5 8.5 10 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 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 = 8.5 8.5 10 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 384 7 3 7 2.6 CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
137636882 156159 None 0 Human Functional pEC50 = 8.5 8.5 - 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 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4062704 156159 None 0 Human Functional pEC50 = 8.5 8.5 - 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 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137638361 156928 None 0 Human Functional pEC50 = 8.5 8.5 - 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 408 4 3 8 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1cccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4071347 156928 None 0 Human Functional pEC50 = 8.5 8.5 - 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 408 4 3 8 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1cccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137662043 159272 None 0 Human Functional pEC50 = 8.5 8.5 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4098394 159272 None 0 Human Functional pEC50 = 8.5 8.5 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137660912 159346 None 0 Human Functional pEC50 = 8.5 8.5 - 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 389 5 2 7 2.5 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4099134 159346 None 0 Human Functional pEC50 = 8.5 8.5 - 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 389 5 2 7 2.5 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137658694 159572 None 0 Human Functional pEC50 = 8.5 8.5 - 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 421 5 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4101617 159572 None 0 Human Functional pEC50 = 8.5 8.5 - 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 421 5 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
124277855 192472 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 325 5 2 5 3.8 CNc1nc(NCc2ccccc2Cl)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
CHEMBL5207240 192472 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 325 5 2 5 3.8 CNc1nc(NCc2ccccc2Cl)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
118716401 114894 None 0 Mouse Functional pEC50 = 8.5 8.5 3 2
Agonist activity at mouse GPR39 by IP1 assayAgonist activity at mouse 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 Mouse Functional pEC50 = 8.5 8.5 3 2
Agonist activity at mouse GPR39 by IP1 assayAgonist activity at mouse 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
118716410 115009 None 0 Mouse Functional pEC50 = 8.5 8.5 5 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 325 5 2 5 3.8 CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342367 115009 None 0 Mouse Functional pEC50 = 8.5 8.5 5 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 325 5 2 5 3.8 CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
3007855 14439 None 35 Human Functional pEC50 = 8.4 8.4 - 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 134 0 0 0 -6.0 [Cl-].[Cl-].[Zn+2] 10.1021/ml500240d
5727 14439 None 35 Human Functional pEC50 = 8.4 8.4 - 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 134 0 0 0 -6.0 [Cl-].[Cl-].[Zn+2] 10.1021/ml500240d
CHEMBL1200679 14439 None 35 Human Functional pEC50 = 8.4 8.4 - 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 134 0 0 0 -6.0 [Cl-].[Cl-].[Zn+2] 10.1021/ml500240d
118716419 115020 None 0 Human Functional pEC50 = 7.5 7.5 -3 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 348 6 3 6 2.6 CNC(=O)c1ccc(CNc2cc(-c3ccccn3)nc(NC)n2)cc1 10.1021/ml500240d
CHEMBL3342378 115020 None 0 Human Functional pEC50 = 7.5 7.5 -3 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 348 6 3 6 2.6 CNC(=O)c1ccc(CNc2cc(-c3ccccn3)nc(NC)n2)cc1 10.1021/ml500240d
137661197 159428 None 1 Human Functional pEC50 = 7.5 7.5 -3 2
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 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 = 7.5 7.5 -3 2
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 451 4 2 9 2.5 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137633165 156411 None 0 Human Functional pEC50 = 5.5 5.5 - 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 473 5 1 6 5.3 Cc1cc(C)nc(-n2nc(C)c3c2NC(=O)CC3c2ccc(COc3cccc(Cl)c3)cc2)n1 10.1021/acs.jmedchem.6b00648
CHEMBL4065636 156411 None 0 Human Functional pEC50 = 5.5 5.5 - 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 473 5 1 6 5.3 Cc1cc(C)nc(-n2nc(C)c3c2NC(=O)CC3c2ccc(COc3cccc(Cl)c3)cc2)n1 10.1021/acs.jmedchem.6b00648
118716411 115010 None 0 Mouse Functional pEC50 = 6.5 6.5 -3 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 292 5 2 6 2.6 CNc1nc(NCc2ccncc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342368 115010 None 0 Mouse Functional pEC50 = 6.5 6.5 -3 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 292 5 2 6 2.6 CNc1nc(NCc2ccncc2)cc(-c2ccccn2)n1 10.1021/ml500240d
76331797 103973 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
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 Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
ChEMBL 423 7 2 4 3.6 CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 10.1021/ml400275z
137642799 158462 None 0 Human Functional pEC50 = 7.5 7.5 - 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 402 3 2 7 1.9 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4089753 158462 None 0 Human Functional pEC50 = 7.5 7.5 - 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 402 3 2 7 1.9 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137661496 159588 None 0 Human Functional pEC50 = 5.5 5.5 - 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 409 3 2 9 1.4 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1nccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4101801 159588 None 0 Human Functional pEC50 = 5.5 5.5 - 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 409 3 2 9 1.4 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1nccs1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716414 115015 None 0 Mouse Functional pEC50 = 7.5 7.5 -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 365 5 2 5 4.7 CNc1nc(NC2(c3ccc(Cl)cc3)CCC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342373 115015 None 0 Mouse Functional pEC50 = 7.5 7.5 -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 365 5 2 5 4.7 CNc1nc(NC2(c3ccc(Cl)cc3)CCC2)cc(-c2ccccn2)n1 10.1021/ml500240d
137641632 158376 None 0 Human Functional pEC50 = 6.5 6.5 - 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 372 5 4 10 -0.2 C=CCN1c2c(n(C)c(=O)n(C)c2=O)NC1N/N=C/c1ccc(O)cc1O 10.1021/acs.jmedchem.6b00648
CHEMBL4088923 158376 None 0 Human Functional pEC50 = 6.5 6.5 - 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 372 5 4 10 -0.2 C=CCN1c2c(n(C)c(=O)n(C)c2=O)NC1N/N=C/c1ccc(O)cc1O 10.1021/acs.jmedchem.6b00648
118716416 115017 None 0 Human Functional pEC50 = 7.4 7.4 5 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 369 6 2 7 2.6 CNc1nc(NCc2ccc(S(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342375 115017 None 0 Human Functional pEC50 = 7.4 7.4 5 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 369 6 2 7 2.6 CNc1nc(NCc2ccc(S(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
118716408 115007 None 0 Mouse Functional pEC50 = 6.4 6.4 -5 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 271 4 2 5 3.0 CNc1nc(NCC(C)(C)C)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342365 115007 None 0 Mouse Functional pEC50 = 6.4 6.4 -5 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 271 4 2 5 3.0 CNc1nc(NCC(C)(C)C)cc(-c2ccccn2)n1 10.1021/ml500240d
135634945 158797 None 6 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse 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 mouse 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 403 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(OC(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4093273 158797 None 6 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse 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 mouse 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 403 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(OC(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137637255 155997 None 0 Human Functional pEC50 = 6.4 6.4 - 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 403 4 2 8 2.0 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4060772 155997 None 0 Human Functional pEC50 = 6.4 6.4 - 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 403 4 2 8 2.0 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137644868 158296 None 0 Human Functional pEC50 = 6.4 6.4 - 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 397 9 2 7 3.6 CCCCCCCCOC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12 10.1021/acs.jmedchem.6b00648
CHEMBL4087979 158296 None 0 Human Functional pEC50 = 6.4 6.4 - 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 397 9 2 7 3.6 CCCCCCCCOC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12 10.1021/acs.jmedchem.6b00648
137636773 155919 None 0 Human Functional pEC50 = 8.4 8.4 - 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 420 4 3 7 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4059978 155919 None 0 Human Functional pEC50 = 8.4 8.4 - 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 420 4 3 7 1.7 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137635316 156229 None 0 Human Functional pEC50 = 8.4 8.4 - 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 407 3 2 8 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4063554 156229 None 0 Human Functional pEC50 = 8.4 8.4 - 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 407 3 2 8 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137631764 156605 None 0 Human Functional pEC50 = 8.4 8.4 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C#N)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4067834 156605 None 0 Human Functional pEC50 = 8.4 8.4 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C#N)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137645445 157629 None 0 Human Functional pEC50 = 8.4 8.4 - 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 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 = 8.4 8.4 - 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 341 4 2 7 1.9 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(C)C)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137646005 157816 None 0 Human Functional pEC50 = 8.4 8.4 - 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(OCc1ccccc1F)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4082109 157816 None 0 Human Functional pEC50 = 8.4 8.4 - 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(OCc1ccccc1F)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137654391 158619 None 0 Human Functional pEC50 = 8.4 8.4 - 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 443 4 2 7 3.8 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(Cl)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4091396 158619 None 0 Human Functional pEC50 = 8.4 8.4 - 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 443 4 2 7 3.8 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(Cl)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716400 114999 None 0 Mouse Functional pEC50 = 8.4 8.4 50 2
Agonist activity at mouse GPR39 by IP1 assayAgonist activity at mouse GPR39 by IP1 assay
ChEMBL 510 10 3 7 4.4 O=S(=O)(NC[C@H]1CC[C@H](CNc2nc(NC3CC3)cc(-c3ccccn3)n2)CC1)c1cccc(F)c1 10.1021/ml500240d
CHEMBL3342357 114999 None 0 Mouse Functional pEC50 = 8.4 8.4 50 2
Agonist activity at mouse GPR39 by IP1 assayAgonist activity at mouse GPR39 by IP1 assay
ChEMBL 510 10 3 7 4.4 O=S(=O)(NC[C@H]1CC[C@H](CNc2nc(NC3CC3)cc(-c3ccccn3)n2)CC1)c1cccc(F)c1 10.1021/ml500240d
137660912 159346 None 0 Human Functional pEC50 = 7.4 7.4 - 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 389 5 2 7 2.5 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4099134 159346 None 0 Human Functional pEC50 = 7.4 7.4 - 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 389 5 2 7 2.5 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137662043 159272 None 0 Human Functional pEC50 = 6.4 6.4 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4098394 159272 None 0 Human Functional pEC50 = 6.4 6.4 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(NC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
76317176 103974 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
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 Functional pEC50 = 5.4 5.4 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
ChEMBL 443 9 1 4 4.1 COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 10.1021/ml400275z
135634948 156517 None 6 Human Functional pEC50 = 6.3 6.3 - 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 381 2 2 6 2.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1F)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4066831 156517 None 6 Human Functional pEC50 = 6.3 6.3 - 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 381 2 2 6 2.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1F)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137648191 157930 None 0 Human Functional pEC50 = 7.3 7.3 - 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 409 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4083614 157930 None 0 Human Functional pEC50 = 7.3 7.3 - 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 409 4 2 7 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
168292047 192048 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in 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 Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 278 4 1 5 3.4 CNc1nc(Oc2ccccc2)cc(-c2ccccn2)n1 10.1016/j.bmcl.2022.128607
118716418 115019 None 0 Human Functional pEC50 = 8.3 8.3 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 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 = 8.3 8.3 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 348 6 3 6 3.2 CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
137648315 157714 None 0 Human Functional pEC50 = 8.3 8.3 - 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 417 5 2 7 3.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4081167 157714 None 0 Human Functional pEC50 = 8.3 8.3 - 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 417 5 2 7 3.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C(C)C)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137647882 157795 None 0 Human Functional pEC50 = 8.3 8.3 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4081885 157795 None 0 Human Functional pEC50 = 8.3 8.3 - 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 402 4 3 7 1.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137644264 158554 None 0 Human Functional pEC50 = 8.3 8.3 - 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 430 5 3 7 2.5 CCC(C(=O)NC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12)c1ccccc1 10.1021/acs.jmedchem.6b00648
CHEMBL4090669 158554 None 0 Human Functional pEC50 = 8.3 8.3 - 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 430 5 3 7 2.5 CCC(C(=O)NC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12)c1ccccc1 10.1021/acs.jmedchem.6b00648
137657821 159886 None 0 Human Functional pEC50 = 8.3 8.3 - 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 394 4 2 9 2.1 Cc1noc(C)c1COC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12 10.1021/acs.jmedchem.6b00648
CHEMBL4105417 159886 None 0 Human Functional pEC50 = 8.3 8.3 - 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 394 4 2 9 2.1 Cc1noc(C)c1COC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12 10.1021/acs.jmedchem.6b00648
135634901 157448 None 33 Mouse Functional pEC50 = 8.3 8.3 1 2
Agonist activity at mouse 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 mouse 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4077818 157448 None 33 Mouse Functional pEC50 = 8.3 8.3 1 2
Agonist activity at mouse 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 mouse 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716403 115002 None 0 Human Functional pEC50 = 5.3 5.3 -3 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 311 6 2 5 3.8 CC(C)(C)CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342360 115002 None 0 Human Functional pEC50 = 5.3 5.3 -3 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 311 6 2 5 3.8 CC(C)(C)CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
137642799 158462 None 0 Human Functional pEC50 = 5.3 5.3 - 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 402 3 2 7 1.9 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4089753 158462 None 0 Human Functional pEC50 = 5.3 5.3 - 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 402 3 2 7 1.9 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)N(C)c1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137637255 155997 None 0 Human Functional pEC50 = 8.2 8.2 - 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 403 4 2 8 2.0 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4060772 155997 None 0 Human Functional pEC50 = 8.2 8.2 - 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 403 4 2 8 2.0 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC(=O)Cc1ccccc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716413 115013 None 0 Human Functional pEC50 = 7.2 7.2 -60 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 393 6 2 5 4.8 FC(F)(F)CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342371 115013 None 0 Human Functional pEC50 = 7.2 7.2 -60 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 393 6 2 5 4.8 FC(F)(F)CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
137631764 156605 None 0 Human Functional pEC50 = 7.2 7.2 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C#N)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4067834 156605 None 0 Human Functional pEC50 = 7.2 7.2 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(C#N)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716405 115004 None 0 Human Functional pEC50 = 6.2 6.2 -27 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 415 8 2 6 4.9 FC(F)(F)Oc1ccc(CNc2nc(NCC3CC3)cc(-c3ccccn3)n2)cc1 10.1021/ml500240d
CHEMBL3342362 115004 None 0 Human Functional pEC50 = 6.2 6.2 -27 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 415 8 2 6 4.9 FC(F)(F)Oc1ccc(CNc2nc(NCC3CC3)cc(-c3ccccn3)n2)cc1 10.1021/ml500240d
137657224 159797 None 0 Human Functional pEC50 = 7.2 7.2 - 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 353 3 2 7 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC1CCCC1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4104345 159797 None 0 Human Functional pEC50 = 7.2 7.2 - 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 353 3 2 7 2.2 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OC1CCCC1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
73211886 1017 None 3 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 10.1016/j.bmcl.2022.128607
7800 1017 None 3 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 10.1016/j.bmcl.2022.128607
CHEMBL3092413 1017 None 3 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 10.1016/j.bmcl.2022.128607
168273327 190676 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 361 4 1 5 4.6 Cc1cc(NC(C)(C)c2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5180126 190676 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 361 4 1 5 4.6 Cc1cc(NC(C)(C)c2ccc(F)cc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
118716407 115006 None 0 Mouse Functional pEC50 = 5.2 5.2 - 1
Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay
ChEMBL 269 5 1 5 2.4 CN(C)c1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342364 115006 None 0 Mouse Functional pEC50 = 5.2 5.2 - 1
Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay
ChEMBL 269 5 1 5 2.4 CN(C)c1nc(NCC2CC2)cc(-c2ccccn2)n1 10.1021/ml500240d
137650161 157232 None 0 Human Functional pEC50 = 8.2 8.2 - 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 446 4 3 9 1.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc3c(c1)OCO3)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4075137 157232 None 0 Human Functional pEC50 = 8.2 8.2 - 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 446 4 3 9 1.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc3c(c1)OCO3)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716415 115016 None 0 Mouse Functional pEC50 = 8.2 8.2 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 375 6 2 6 4.1 CNc1nc(NCc2ccc(OC(F)(F)F)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342374 115016 None 0 Mouse Functional pEC50 = 8.2 8.2 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 375 6 2 6 4.1 CNc1nc(NCc2ccc(OC(F)(F)F)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
137643474 158393 None 0 Human Functional pEC50 = 7.2 7.2 - 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 419 6 2 8 2.5 COc1ccc(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)cc1 10.1021/acs.jmedchem.6b00648
CHEMBL4089047 158393 None 0 Human Functional pEC50 = 7.2 7.2 - 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 419 6 2 8 2.5 COc1ccc(CCOC2CC(=O)Nc3c2c(C)nn3-c2ncnc3nc[nH]c23)cc1 10.1021/acs.jmedchem.6b00648
118716408 115007 None 0 Human Functional pEC50 = 7.1 7.1 5 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 271 4 2 5 3.0 CNc1nc(NCC(C)(C)C)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342365 115007 None 0 Human Functional pEC50 = 7.1 7.1 5 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 271 4 2 5 3.0 CNc1nc(NCC(C)(C)C)cc(-c2ccccn2)n1 10.1021/ml500240d
9586016 108470 None 8 Human Functional pEC50 = 6.1 6.1 - 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 365 8 5 9 2.1 OCC(O)/C=N/Nc1nc(Nc2ccccc2)nc(Nc2ccccc2)n1 10.1021/acs.jmedchem.6b00648
CHEMBL3198662 108470 None 8 Human Functional pEC50 = 6.1 6.1 - 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 365 8 5 9 2.1 OCC(O)/C=N/Nc1nc(Nc2ccccc2)nc(Nc2ccccc2)n1 10.1021/acs.jmedchem.6b00648
137646005 157816 None 0 Human Functional pEC50 = 7.1 7.1 - 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 393 4 2 7 2.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1F)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4082109 157816 None 0 Human Functional pEC50 = 7.1 7.1 - 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 393 4 2 7 2.6 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1F)CC(=O)N2 10.1021/acs.jmedchem.6b00648
168277952 190769 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 390 5 2 6 3.1 CNC(=O)C(Nc1cc(C)nc2c(-c3ccccn3)cnn12)c1ccc(F)cc1 10.1016/j.bmcl.2022.128607
CHEMBL5181574 190769 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 390 5 2 6 3.1 CNC(=O)C(Nc1cc(C)nc2c(-c3ccccn3)cnn12)c1ccc(F)cc1 10.1016/j.bmcl.2022.128607
137644264 158554 None 0 Human Functional pEC50 = 7.1 7.1 - 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 430 5 3 7 2.5 CCC(C(=O)NC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12)c1ccccc1 10.1021/acs.jmedchem.6b00648
CHEMBL4090669 158554 None 0 Human Functional pEC50 = 7.1 7.1 - 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 430 5 3 7 2.5 CCC(C(=O)NC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12)c1ccccc1 10.1021/acs.jmedchem.6b00648
168276005 190740 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 356 3 0 6 3.8 Cc1cc(N2CCCC2c2cccnc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
CHEMBL5181167 190740 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ fluxAgonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
ChEMBL 356 3 0 6 3.8 Cc1cc(N2CCCC2c2cccnc2)n2ncc(-c3ccccn3)c2n1 10.1016/j.bmcl.2022.128607
137650161 157232 None 0 Human Functional pEC50 = 6.1 6.1 - 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 446 4 3 9 1.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc3c(c1)OCO3)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4075137 157232 None 0 Human Functional pEC50 = 6.1 6.1 - 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 446 4 3 9 1.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)NCc1ccc3c(c1)OCO3)CC(=O)N2 10.1021/acs.jmedchem.6b00648
137644868 158296 None 0 Human Functional pEC50 = 8.1 8.1 - 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 397 9 2 7 3.6 CCCCCCCCOC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12 10.1021/acs.jmedchem.6b00648
CHEMBL4087979 158296 None 0 Human Functional pEC50 = 8.1 8.1 - 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 397 9 2 7 3.6 CCCCCCCCOC1CC(=O)Nc2c1c(C)nn2-c1ncnc2nc[nH]c12 10.1021/acs.jmedchem.6b00648
137658295 159813 None 0 Human Functional pEC50 = 8.1 8.1 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1C#N)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4104470 159813 None 0 Human Functional pEC50 = 8.1 8.1 - 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 400 4 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccccc1C#N)CC(=O)N2 10.1021/acs.jmedchem.6b00648
118716417 115018 None 0 Mouse Functional pEC50 = 8.1 8.1 -10 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 384 7 3 7 2.6 CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342376 115018 None 0 Mouse Functional pEC50 = 8.1 8.1 -10 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 384 7 3 7 2.6 CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
118716419 115020 None 0 Mouse Functional pEC50 = 8.1 8.1 3 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 348 6 3 6 2.6 CNC(=O)c1ccc(CNc2cc(-c3ccccn3)nc(NC)n2)cc1 10.1021/ml500240d
CHEMBL3342378 115020 None 0 Mouse Functional pEC50 = 8.1 8.1 3 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 348 6 3 6 2.6 CNC(=O)c1ccc(CNc2cc(-c3ccccn3)nc(NC)n2)cc1 10.1021/ml500240d
3395869 115014 None 0 Human Functional pEC50 = 7.1 7.1 -4 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 310 4 1 4 4.1 Cc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342372 115014 None 0 Human Functional pEC50 = 7.1 7.1 -4 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 310 4 1 4 4.1 Cc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 10.1021/ml500240d
76313672 103972 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
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 Functional pEC50 = 6.1 6.1 - 1
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 minsAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
ChEMBL 423 7 2 4 3.6 CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 10.1021/ml400275z
118716411 115010 None 0 Human Functional pEC50 = 7.1 7.1 3 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 292 5 2 6 2.6 CNc1nc(NCc2ccncc2)cc(-c2ccccn2)n1 10.1021/ml500240d
CHEMBL3342368 115010 None 0 Human Functional pEC50 = 7.1 7.1 3 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 292 5 2 6 2.6 CNc1nc(NCc2ccncc2)cc(-c2ccccn2)n1 10.1021/ml500240d
135634901 157448 None 33 Human Functional pEC50 = 8.1 8.1 -1 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4077818 157448 None 33 Human Functional pEC50 = 8.1 8.1 -1 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 397 2 2 6 3.1 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(c1ccc(F)cc1Cl)CC(=O)N2 10.1021/acs.jmedchem.6b00648
73211886 1017 None 3 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by FLIPR assayAgonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by 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 Functional pEC50 = 6.1 6.1 - 1
Agonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by FLIPR assayAgonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by 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 Functional pEC50 = 6.1 6.1 - 1
Agonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by FLIPR assayAgonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by FLIPR assay
ChEMBL 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 10.1021/ml400275z
137658694 159572 None 0 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 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 421 5 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
CHEMBL4101617 159572 None 0 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 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 421 5 2 8 2.3 Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(=O)c1ccc(F)cc1)CC(=O)N2 10.1021/acs.jmedchem.6b00648
73211886 1017 None 3 Human Functional pEC50 = 6.1 6.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 24900608
7800 1017 None 3 Human Functional pEC50 = 6.1 6.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 24900608
CHEMBL3092413 1017 None 3 Human Functional pEC50 = 6.1 6.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 24900608
7803 993 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 359 5 2 5 4.5 CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 25313322
86277841 993 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 359 5 2 5 4.5 CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 25313322
CHEMBL3342370 993 None 0 Human Functional pEC50 = 9.1 9.1 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 359 5 2 5 4.5 CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 25313322


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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
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