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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]