compound 1 [PMID: 24900608] [Ligand Id: 7800] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3092413
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  • phosphodiesterase 3A/Phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
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  • phosphodiesterase 3B/Phosphodiesterase 3B in Human [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR39/G-protein coupled receptor 39 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091266] [GtoPdb: 105] [UniProtKB: O43194]
ChEMBL 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 mins F 4.92 pEC50 12000 nM EC50 ACS Med Chem Lett (2013) 4: 1079-1084 [PMID:24900608]
ChEMBL Agonist activity at GPR39 in human HT-29 cells assessed as increase in intracellular Ca2+ mobilization after 72 hrs by FLIPR assay F 6.05 pEC50 900 nM EC50 ACS Med Chem Lett (2013) 4: 1079-1084 [PMID:24900608]
GtoPdb - - 7.2 pEC50 59 nM EC50 ACS Med Chem Lett (2013) 4: 1079-84 [PMID:24900608]
ChEMBL 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 assay B 7.25 pEC50 56 nM EC50 ACS Med Chem Lett (2013) 4: 1079-1084 [PMID:24900608]
phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
ChEMBL Inhibition of PDE3a (unknown origin) B 4.82 pIC50 15000 nM IC50 ACS Med Chem Lett (2013) 4: 1079-1084 [PMID:24900608]
phosphodiesterase 3B/Phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
ChEMBL Inhibition of PDE3B (unknown origin) B 4.62 pIC50 24000 nM IC50 ACS Med Chem Lett (2013) 4: 1079-1084 [PMID:24900608]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]