ibudilast [Ligand Id: 7399] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL19449 (Ibudilast, AV411, MN-166, AV-411)
  • 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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  • phosphodiesterase 3A in Human [GtoPdb: 1298] [UniProtKB: Q14432]
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  • phosphodiesterase 5A in Human [GtoPdb: 1304] [UniProtKB: O76074]
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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 5.89 pIC50 1300 nM IC50 J. Med. Chem. (2011) 54: 3331-3347 [PMID:21456625]
ChEMBL Inhibition of human PDE4A B 7.27 pIC50 54 nM IC50 J. Med. Chem. (2008) 51: 5471-5489 [PMID:18686943]
GtoPdb - - 7.27 pIC50 54 nM IC50 J Med Chem (2008) 51: 5471-89 [PMID:18686943]
ChEMBL Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci B 6.05 pEC50 900 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 PDE4B catalytic domain using cAMP/cGMP substrate B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3307-3312 [PMID:21530250]
ChEMBL Inhibition of human PDE4B B 7.19 pIC50 65 nM IC50 J. Med. Chem. (2008) 51: 5471-5489 [PMID:18686943]
GtoPdb - - 7.19 pIC50 65 nM IC50 J Med Chem (2008) 51: 5471-89 [PMID:18686943]
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb - - 6.62 pIC50 239 nM IC50 J Med Chem (2008) 51: 5471-89 [PMID:18686943]
ChEMBL Inhibition of human PDE4C B 6.62 pIC50 239 nM IC50 J. Med. Chem. (2008) 51: 5471-5489 [PMID:18686943]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL Inhibition of human PDE4D B 6.78 pIC50 166 nM IC50 J. Med. Chem. (2008) 51: 5471-5489 [PMID:18686943]
phosphodiesterase 3A in Human [GtoPdb: 1298] [UniProtKB: Q14432]
GtoPdb - - 3.52 pIC50 299000 nM IC50 Bioorg Med Chem Lett (2011) 21: 3307-12 [PMID:21530250]
phosphodiesterase 5A in Human [GtoPdb: 1304] [UniProtKB: O76074]
GtoPdb - - 3.99 pIC50 103000 nM IC50 Bioorg Med Chem Lett (2011) 21: 3307-12 [PMID:21530250]

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]