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 |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 4A/3`,5`-cyclic-AMP 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] |
| ChEMBL | Affinity Biochemical interaction: (Inhibition of radiolabelled [3H]cAMP cleavage) EUB0002598a PDE4A | F | 7.27 | pIC50 | 54 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| 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/3`,5`-cyclic-AMP 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] |
| ChEMBL | Affinity Biochemical interaction: (Inhibition of radiolabelled [3H]cAMP cleavage) EUB0002598a PDE4B | F | 7.19 | pIC50 | 65 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 7.19 | pIC50 | 65 | nM | IC50 | J Med Chem (2008) 51: 5471-89 [PMID:18686943] |
| phosphodiesterase 4C/3`,5`-cyclic-AMP 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] |
| ChEMBL | Affinity Biochemical interaction: (Inhibition of radiolabelled [3H]cAMP cleavage) EUB0002598a PDE4C | F | 6.62 | pIC50 | 239 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| phosphodiesterase 4D/3`,5`-cyclic-AMP 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] |
| ChEMBL | Affinity Biochemical interaction: (Inhibition of radiolabelled [3H]cAMP cleavage) EUB0002598a PDE4D | F | 6.78 | pIC50 | 166 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic 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 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] | ||||||||
| GtoPdb | - | - | 3.52 | pIC50 | 299000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3307-12 [PMID:21530250] |
| ChEMBL | Selectivity interaction (Enzymatic assay) EUB0002598a PDE3A | B | 5.8 | pIC50 | 1600 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphodiesterase 3B/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370] | ||||||||
| ChEMBL | Selectivity interaction (Enzymatic assay) EUB0002598a PDE3B | B | 5.57 | pIC50 | 2700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphodiesterase 5A/cGMP-specific 3`,5`-cyclic phosphodiesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| GtoPdb | - | - | 3.99 | pIC50 | 103000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3307-12 [PMID:21530250] |
| ChEMBL | Selectivity interaction (Enzymatic assay) EUB0002598a PDE5A | B | 5.45 | pIC50 | 3510 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Enzymatic assay) EUB0002598a PDE5A | B | 5.45 | pIC50 | 3510 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphodiesterase 11A/Dual 3`,5`-cyclic-AMP and -GMP 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] |
| 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] |
ChEMBL data shown on this page come from version 36:
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]
