amlexanox [Ligand Id: 7113] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1096 (AA-673, Amlexanox, Amoxanox, Aphthasol, Aphtheal, CHX 3673, CHX-3673, Elics, Solfa)
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  • inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
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  • Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
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  • TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL Agonist activity at human GPR35 expressed in CHO-K1 cells after 90 mins by beta-arrestin 2 recruitment assay B 5.4 pEC50 4000 nM EC50 J Med Chem (2017) 60: 362-372 [PMID:27976894]
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
ChEMBL Inhibition of human IKKepsilon (1 to 655 residues) expressed in Baculovirus infected SF9 insect cells using myelin basic protein as substrate in presence of [gamma-33P]-ATP by radiometric kinase assay B 5.29 pIC50 5128.61 nM IC50 Bioorg Med Chem (2018) 26: 5443-5461 [PMID:30270002]
ChEMBL Inhibition of human IKKepsilon (1 to 655 residues) expressed in Baculovirus infected SF9 insect cells using myelin basic protein as substrate in presence of [gamma-33P]-ATP by radiometric kinase assay B 5.29 pIC50 5100 nM IC50 Bioorg Med Chem (2018) 26: 5443-5461 [PMID:30270002]
GtoPdb Inhibition of substrate phosphorylation. - 6 pIC50 1000 nM IC50 Nat Med (2013) 19: 313-21 [PMID:23396211]
Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
ChEMBL MERS_3CL Pro protease inhibition IC50 by FRET kind of response from peptide substrate F 5 pIC50 >10000 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
GtoPdb Inhibition of substrate phosphorylation. - 6 pIC50 1000 nM IC50 Nat Med (2013) 19: 313-21 [PMID:23396211]
ChEMBL Inhibition of human TBK1 (1 to 657 residues) expressed in Baculovirus infected SF9 insect cells using myelin basic protein as substrate in presence of [gamma-33P]-ATP by radiometric kinase assay B 6.07 pIC50 851.14 nM IC50 Bioorg Med Chem (2018) 26: 5443-5461 [PMID:30270002]
ChEMBL Inhibition of human TBK1 (1 to 657 residues) expressed in Baculovirus infected SF9 insect cells using myelin basic protein as substrate in presence of [gamma-33P]-ATP by radiometric kinase assay B 6.07 pIC50 850 nM IC50 Bioorg Med Chem (2018) 26: 5443-5461 [PMID:30270002]
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
ChEMBL Binding affinity to TTR V3OM mutant (unknown origin) expressed in Escherichia coli incubated for 60 mins by tryptophan intrinsic fluorescence method B 4.7 pKd 20000 nM Kd J Med Chem (2021) 64: 14344-14357 [PMID:34547896]

ChEMBL data shown on this page come from version 33:

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]