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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL32442
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
There should be some charts here, you may need to enable JavaScript!
  • 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 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [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 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 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]