RS-25344 [Ligand Id: 6557] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1232082
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 4B in Human [GtoPdb: 1301] [UniProtKB: Q07343]
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  • phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D in Human [GtoPdb: 1303] [UniProtKB: Q08499]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
GtoPdb - - 7.2 pIC50 - - - Cell Signal (1998) 10: 427-40 [PMID:9720765]
ChEMBL Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay B 7.66 pIC50 22 nM IC50 J Med Chem (2011) 54: 3331-3347 [PMID:21456625]
ChEMBL Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci B 7.77 pEC50 17 nM EC50 J Med Chem (2011) 54: 3331-3347 [PMID:21456625]
phosphodiesterase 4B in Human [GtoPdb: 1301] [UniProtKB: Q07343]
GtoPdb - - 6.5 pIC50 - - - Cell Signal (1998) 10: 427-40 [PMID:9720765]
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb - - 8.1 pIC50 - - - Cell Signal (1998) 10: 427-40 [PMID:9720765]
phosphodiesterase 4D in Human [GtoPdb: 1303] [UniProtKB: Q08499]
GtoPdb - - 8.4 pIC50 - - - Cell Signal (1998) 10: 427-40 [PMID:9720765]

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]