apremilast [Ligand Id: 7372] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL514800 (Apremilast, CC-10004, CC10004, Otezla)
  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
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  • phosphodiesterase 4A in Human [GtoPdb: 1300] [UniProtKB: P27815]
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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 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL Inhibition of recombinant human PDE4B2 expressed in African green monkey COS7 cells using cAMP as substrate B 7.52 pIC50 30 nM IC50 J Med Chem (2018) 61: 2472-2489 [PMID:29502405]
GtoPdb Potency against recombinant human PDE4B1 and B2 isoforms in a TR-FRET assay. - 7.57 pIC50 27 nM IC50 Cell. Signal. (2014) 26: 2016-29 [PMID:24882690]
phosphodiesterase 4A in Human [GtoPdb: 1300] [UniProtKB: P27815]
GtoPdb Potency against recombinant human PDE4A1A isoform in a TR-FRET assay. - 7.85 pIC50 14 nM IC50 Cell. Signal. (2014) 26: 2016-29 [PMID:24882690]
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb Potency against recombinant human PDE4C1 isoform in a TR-FRET assay. - 6.93 pIC50 118 nM IC50 Cell. Signal. (2014) 26: 2016-29 [PMID:24882690]
phosphodiesterase 4D in Human [GtoPdb: 1303] [UniProtKB: Q08499]
GtoPdb Potency against recombinant human PDE4D2 isoform in a TR-FRET assay. - 7.48 pIC50 33 nM IC50 Cell. Signal. (2014) 26: 2016-29 [PMID:24882690]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]