Ligand source activities (1 row/activity)



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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

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weight		 Rot
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 DOI
91826086 114936 47 None - 1 Human 10.2 pEC50 = 10.2 Functional
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 114936 47 None - 1 Human 10.2 pEC50 = 10.2 Functional
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 114954 0 None 10 2 Human 9.7 pEC50 = 9.7 Functional
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 114954 0 None 10 2 Human 9.7 pEC50 = 9.7 Functional
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 114957 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 114957 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 0 None 1 2 Mouse 9.3 pEC50 = 9.3 Functional
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 0 None 1 2 Mouse 9.3 pEC50 = 9.3 Functional
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 0 None 1 2 Mouse 9.3 pEC50 = 9.3 Functional
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 114955 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
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 114955 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
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 114936 47 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 114936 47 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
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 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
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 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
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 114936 47 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 114936 47 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 114957 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 114957 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 156896 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 156896 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 114949 0 None 60 2 Mouse 9.0 pEC50 = 9 Functional
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 114949 0 None 60 2 Mouse 9.0 pEC50 = 9 Functional
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 159334 1 None -3 2 Human 8.8 pEC50 = 8.8 Functional
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 159334 1 None -3 2 Human 8.8 pEC50 = 8.8 Functional
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 156581 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 156581 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 158098 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 158098 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 114944 0 None 1 2 Mouse 8.0 pEC50 = 8 Functional
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 114944 0 None 1 2 Mouse 8.0 pEC50 = 8 Functional
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 114939 0 None -4 2 Mouse 5.0 pEC50 = 5 Functional
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 114939 0 None -4 2 Mouse 5.0 pEC50 = 5 Functional
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 114941 0 None 2 2 Mouse 5.0 pEC50 = 5 Functional
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 114941 0 None 2 2 Mouse 5.0 pEC50 = 5 Functional
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 114830 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
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 114830 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
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 114944 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
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 114944 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
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 155904 13 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 155904 13 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 157537 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 157537 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 114937 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
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 114937 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
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 114947 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 114947 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 159334 1 None -3 2 Human 7.9 pEC50 = 7.9 Functional
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 159334 1 None -3 2 Human 7.9 pEC50 = 7.9 Functional
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 3 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 3 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 3 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 155829 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 155829 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 156896 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 156896 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 159719 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 159719 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 114952 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
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 114952 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
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 114945 1 None -5 2 Human 7.8 pEC50 = 7.8 Functional
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 114945 1 None -5 2 Human 7.8 pEC50 = 7.8 Functional
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 114936 47 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 114936 47 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 190738 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 190738 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 114938 0 None 3 2 Mouse 5.8 pEC50 = 5.8 Functional
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 114938 0 None 3 2 Mouse 5.8 pEC50 = 5.8 Functional
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 156068 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 156068 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 157428 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 157428 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159035 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159035 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 191641 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 191641 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 158098 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 158098 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 114937 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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 114937 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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 157622 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 157622 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 157356 33 None -1 2 Human 7.8 pEC50 = 7.8 Functional
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 157356 33 None -1 2 Human 7.8 pEC50 = 7.8 Functional
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 190383 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 190383 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 191430 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 191430 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 114950 1 None 4 2 Mouse 7.8 pEC50 = 7.8 Functional
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 114950 1 None 4 2 Mouse 7.8 pEC50 = 7.8 Functional
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 158705 7 None 1 2 Human 7.8 pEC50 = 7.8 Functional
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 158705 7 None 1 2 Human 7.8 pEC50 = 7.8 Functional
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 159494 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159494 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 157356 33 None 1 2 Mouse 6.8 pEC50 = 6.8 Functional
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 157356 33 None 1 2 Mouse 6.8 pEC50 = 6.8 Functional
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 114953 0 None -5 2 Mouse 6.7 pEC50 = 6.7 Functional
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 114953 0 None -5 2 Mouse 6.7 pEC50 = 6.7 Functional
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 157838 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 157838 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 158301 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 158301 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 159703 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 159703 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 114955 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
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 114955 0 None -1 2 Mouse 8.7 pEC50 = 8.7 Functional
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 159334 1 None 3 2 Mouse 8.6 pEC50 = 8.6 Functional
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 159334 1 None 3 2 Mouse 8.6 pEC50 = 8.6 Functional
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 158721 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 158721 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 157428 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 157428 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 114935 0 None -50 2 Human 6.7 pEC50 = 6.7 Functional
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 114935 0 None -50 2 Human 6.7 pEC50 = 6.7 Functional
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 114940 0 None 27 2 Mouse 7.7 pEC50 = 7.7 Functional
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 114940 0 None 27 2 Mouse 7.7 pEC50 = 7.7 Functional
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 114941 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
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 114941 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
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 114939 0 None 4 2 Human 5.7 pEC50 = 5.7 Functional
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 114939 0 None 4 2 Human 5.7 pEC50 = 5.7 Functional
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 159035 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 159035 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 156654 11 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 156654 11 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 190631 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 190631 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 158527 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 158527 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 156836 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 156836 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 156138 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 156138 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 114951 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
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 114951 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
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 190383 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 190383 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 114947 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
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 114947 0 None -2 2 Mouse 5.6 pEC50 = 5.6 Functional
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 158705 7 None 1 2 Human 5.6 pEC50 = 5.6 Functional
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 158705 7 None 1 2 Human 5.6 pEC50 = 5.6 Functional
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 157356 33 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 157356 33 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 157703 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 157703 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 114954 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
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 114954 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
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 156068 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 156068 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 156836 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 156836 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 159179 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 159179 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 159253 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 159253 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 159478 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 159478 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 192363 1 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 192363 1 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 114830 0 None 3 2 Mouse 8.5 pEC50 = 8.5 Functional
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 114830 0 None 3 2 Mouse 8.5 pEC50 = 8.5 Functional
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 114945 1 None 5 2 Mouse 8.5 pEC50 = 8.5 Functional
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 114945 1 None 5 2 Mouse 8.5 pEC50 = 8.5 Functional
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 14434 62 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 14434 62 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 14434 62 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 114956 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
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 114956 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
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 159334 1 None -3 2 Human 7.5 pEC50 = 7.5 Functional
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 159334 1 None -3 2 Human 7.5 pEC50 = 7.5 Functional
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 156320 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 156320 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 114946 0 None -3 2 Mouse 6.5 pEC50 = 6.5 Functional
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 114946 0 None -3 2 Mouse 6.5 pEC50 = 6.5 Functional
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 103918 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 103918 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 158370 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 158370 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 159494 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 159494 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 114951 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
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 114951 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
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 158284 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 158284 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 114953 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
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 114953 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
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 114943 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
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 114943 0 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
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 158705 7 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
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 158705 7 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
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 155907 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 155907 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 158204 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 158204 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 155829 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 155829 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 156138 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 156138 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 156514 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 156514 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 157537 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 157537 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 157724 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 157724 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 158527 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 158527 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 114935 0 None 50 2 Mouse 8.4 pEC50 = 8.4 Functional
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 114935 0 None 50 2 Mouse 8.4 pEC50 = 8.4 Functional
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 159253 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 159253 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 159179 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 159179 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 103919 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 103919 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 156426 7 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 156426 7 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 157838 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 157838 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 191939 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 191939 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 114955 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
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 114955 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
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 157622 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 157622 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 157703 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 157703 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 158462 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 158462 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 159792 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 159792 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 157356 33 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
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 157356 33 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
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 114938 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
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 114938 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
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 158370 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 158370 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 155907 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 155907 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 114949 0 None -60 2 Human 7.2 pEC50 = 7.2 Functional
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 114949 0 None -60 2 Human 7.2 pEC50 = 7.2 Functional
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 156514 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 156514 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 114940 0 None -27 2 Human 6.2 pEC50 = 6.2 Functional
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 114940 0 None -27 2 Human 6.2 pEC50 = 6.2 Functional
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 159703 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 159703 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 190567 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 190567 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 114942 0 None - 1 Mouse 5.2 pEC50 = 5.2 Functional
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 114942 0 None - 1 Mouse 5.2 pEC50 = 5.2 Functional
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 157140 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 157140 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 114952 0 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
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 114952 0 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
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 158301 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 158301 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 114943 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
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 114943 0 None 5 2 Human 7.1 pEC50 = 7.1 Functional
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 108414 9 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 108414 9 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 157724 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 157724 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 190660 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 190660 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158462 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158462 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 190631 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 190631 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 157140 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 157140 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 158204 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 158204 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 159719 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 159719 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 114954 0 None -10 2 Mouse 8.1 pEC50 = 8.1 Functional
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 114954 0 None -10 2 Mouse 8.1 pEC50 = 8.1 Functional
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 114956 0 None 3 2 Mouse 8.1 pEC50 = 8.1 Functional
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 114956 0 None 3 2 Mouse 8.1 pEC50 = 8.1 Functional
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 114950 1 None -4 2 Human 7.1 pEC50 = 7.1 Functional
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 114950 1 None -4 2 Human 7.1 pEC50 = 7.1 Functional
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 103917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 103917 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 114946 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
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 114946 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
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 157356 33 None -1 2 Human 8.1 pEC50 = 8.1 Functional
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 157356 33 None -1 2 Human 8.1 pEC50 = 8.1 Functional
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 3 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 3 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 3 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 159478 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 159478 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 3 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 24900608
7800 1017 3 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 24900608
CHEMBL3092413 1017 3 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 3 0 6 2.6 N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl 24900608
7803 993 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 359 5 2 5 4.5 CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 25313322
86277841 993 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 359 5 2 5 4.5 CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 25313322
CHEMBL3342370 993 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
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 Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

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weight		 Rot
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 DOI
168269293 189973 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 189973 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 103917 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 103917 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 191939 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 191939 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 191479 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 191479 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 189973 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 189973 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 103919 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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 103919 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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 103918 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 103918 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 190615 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 190615 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 191610 1 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 191610 1 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 3 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 3 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 3 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 192108 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 192108 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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