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 human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux F 5.2 pEC50 6250 nM EC50 Bioorg Med Chem Lett (2022) 61: 128607-128607 [PMID:35123006]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]