apremilast | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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Ligand Activity Charts

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] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4A in Human [GtoPdb: 1300] [UniProtKB: P27815] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4D in Human [GtoPdb: 1303] [UniProtKB: Q08499] There should be some charts here, you may need to enable JavaScript!

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]