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

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ChEMBL ligand: CHEMBL19449 (AV411, AV-411, Ibudilast, Ketas, MN-166)
  • Macrophage migration inhibitory factor in Human [ChEMBL: CHEMBL2085] [UniProtKB: P14174]
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  • 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
Macrophage migration inhibitory factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2085] [UniProtKB: P14174]
ChEMBL Binding affinity to recombinant biotinylated human MIF expressed in Escherichia coli BL21 DE3 by surface plasmon resonance assay B 5.85 pKd 1400 nM Kd ACS Med Chem Lett (2020) 11: 1843-1847 [PMID:33062162]
ChEMBL Non-competitive inhibition of recombinant human MIF assessed as inhibition constant using varying levels of p-hydroxyphenylpyruvate as substrate by Lineweaver-Burk plot analysis B 4.51 pKi 30900 nM Ki ACS Med Chem Lett (2020) 11: 1843-1847 [PMID:33062162]
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]
ChEMBL Inhibition of human PDE4A expressed in insect sf9 cells using [3H]-cAMP as substrate B 7.27 pIC50 54 nM IC50 J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
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]
ChEMBL Inhibition of human PDE4B expressed in insect sf9 cells using [3H]-cAMP as substrate B 7.19 pIC50 65 nM IC50 J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
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]
ChEMBL Inhibition of human PDE4C expressed in insect sf9 cells using [3H]-cAMP as substrate B 6.62 pIC50 239 nM IC50 J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
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]
ChEMBL Inhibition of human PDE4D expressed in insect sf9 cells using [3H]-cAMP as substrate B 6.78 pIC50 166 nM IC50 J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
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 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]