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

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ChEMBL ligand: CHEMBL1096 (Amlexanox, AA-673, CHX-3673, Aphthasol)
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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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  • 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]
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]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]