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ChEMBL ligand: CHEMBL514800 (Apremilast, CC-10004, CC10004, Otezla) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]