CDP840 [Ligand Id: 9330] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL32442
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
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  • phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [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 Inhibition of [3H]-R-rolipram binding to recombinant human PDE-4 isoenzyme - 8.01 pKi 9.7 nM Ki Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241]
ChEMBL Inhibition of recombinant human PDE4A expressed in Sf9 cells B 8.4 pKi 4 nM Ki J. Med. Chem. (2000) 43: 3820-3823 [PMID:11052785]
ChEMBL Inhibitory concentration of compound against LPS- induced TNF-alpha production in whole human blood assay F 4.8 pIC50 16000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1457-1461 [PMID:12031319]
ChEMBL Inhibition of recombinant human PDE4A expressed in Sf9 cells B 5 pIC50 10000 nM IC50 J. Med. Chem. (2000) 43: 3820-3823 [PMID:11052785]
ChEMBL In vitro inhibitory activity was determined against human Phosphodiesterase 4 isoform using a construct representing the common region of spliced variants expressed as a GST-fusion protein in Sf 9 cells B 8.37 pIC50 4.3 nM IC50 J. Med. Chem. (2003) 46: 2413-2426 [PMID:12773045]
ChEMBL Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells B 8.37 pIC50 4.3 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1457-1461 [PMID:12031319]
ChEMBL Inhibition of GST-tagged PDE4A B 8.38 pIC50 4.2 nM IC50 J. Med. Chem. (2008) 51: 5471-5489 [PMID:18686943]
ChEMBL Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells. B 8.38 pIC50 4.2 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 3009-3013 [PMID:12270195]
ChEMBL Inhibition of Phosphodiesterase-4A (PDE4) B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1923-1926 [PMID:12749899]
ChEMBL Inhibition of human recombinant phosphodiesterase 4A B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1451-1456 [PMID:12031318]
ChEMBL Inhibitory activity against PDE4A B 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
GtoPdb Inhibition of [3H]-R-rolipram binding to recombinant human PDE4B2 isoenzyme - 8.07 pKi 8.5 nM Ki Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241]
ChEMBL Inhibitory activity against PDE4B B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb Inhibition of [3H]-R-rolipram binding to recombinant human PDE4C2 isoenzyme - 7.72 pKi 18.9 nM Ki Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241]
ChEMBL Inhibitory activity against PDE4C B 8.35 pIC50 4.5 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
GtoPdb Inhibition of [3H]-R-rolipram binding to recombinant human PDE4D3 isoenzyme - 8.15 pKi 7.1 nM Ki Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241]
ChEMBL Inhibitory activity against PDE4D B 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]

ChEMBL data shown on this page come from version 28:

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]