ibudilast [Ligand Id: 7399] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19449 (AV-411, AV411, Ibudilast, Ketas, MN-166) |
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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 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
| ChEMBL | Inhibition of human PDE10 | B | 5 | pIC50 | <=10000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9] | ||||||||
| ChEMBL | Inhibition of human PDE11 | B | 5 | pIC50 | <=10000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| 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 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]
