Ro20-1724 [Ligand Id: 5258] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL18701 (Ro-201724)
  • 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 in Human [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D in Human [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]
ChEMBL Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay B 5.37 pIC50 4300 nM IC50 J Med Chem (2011) 54: 3331-3347 [PMID:21456625]
GtoPdb - - 6.5 pIC50 316 nM IC50 Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268]
ChEMBL Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci B 5.48 pEC50 3300 nM EC50 J Med Chem (2011) 54: 3331-3347 [PMID:21456625]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL Inhibition of human Phosphodiesterase 4B B 5.71 pKi 1930 nM Ki J Med Chem (1995) 38: 4848-4854 [PMID:7490734]
GtoPdb - - 6.4 pIC50 398 nM IC50 Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268]
TNF-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1825] [UniProtKB: P01375]
ChEMBL TNF-alpha production in PBMC by ELISA method F 4.3 pIC50 50000 nM IC50 J Med Chem (1996) 39: 2-9 [PMID:8568809]
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb - - 5.4 pIC50 3980 nM IC50 Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268]
phosphodiesterase 4D in Human [GtoPdb: 1303] [UniProtKB: Q08499]
GtoPdb - - 6.2 pIC50 631 nM IC50 Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268]

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]