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 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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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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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 human PDE4B using [3H]cAMP as substrate incubated for 5 mins followed by substrate addition and measured after 10 mins by scintillation proximity assay B 7.13 pIC50 74 nM IC50 Bioorg Med Chem (2016) 24: 5702-5716 [PMID:27713015]
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]
ChEMBL Inhibition of PDE4B (unknown origin) B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2019) 174: 198-215 [PMID:31035240]
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 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL Inhibition of PDE4D2 (unknown origin) B 6.27 pIC50 540 nM IC50 J Med Chem (2020) 63: 3370-3380 [PMID:32115956]
ChEMBL Inhibition of PDE4D (unknown origin) using cAMP as substrate B 7.13 pIC50 74 nM IC50 J Med Chem (2019) 62: 5579-5593 [PMID:31099559]
ChEMBL Inhibition of human PDE4D catalytic domain (86 to 413 residues) expressed in Escherichia coli BL21 (DE3) cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay B 7.32 pIC50 47.6 nM IC50 J Nat Prod (2020) 83: 1229-1237 [PMID:32100544]
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 Inhibition of PDE4D (unknown origin) B 7.48 pIC50 33 nM IC50 Eur J Med Chem (2019) 174: 198-215 [PMID:31035240]
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]

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]