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ChEMBL ligand: CHEMBL19449 (AV411, AV-411, Ibudilast, Ketas, MN-166) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 31:
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]