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ChEMBL ligand: CHEMBL2031465 (AZ-12012199, AZ12012199, Azd 6703, Azd-6703, Azd6703, AZD-6703) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-3883 [PMID:22608965] |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | Inhibition of p38alpha in human PBMC assessed as increase in LPS-induced ATF2 phosphorylation stimulated with LPS for 35 mins followed by compound treatment measured after 1 hr in presence of ATP by Western blot analysis | B | 7.3 | pIC50 | 50.12 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127412-127412 [PMID:32717614] |
ChEMBL | Inhibition of p38alpha-mediated TNFalpha secretion in LPS-stimulated human whole blood | B | 7.56 | pIC50 | 27.54 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-3883 [PMID:22608965] |
ChEMBL | Inhibition of p38alpha-mediated TNFalpha secretion in LPS-stimulated human whole blood | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-3883 [PMID:22608965] |
ChEMBL | Inhibition of p38alpha MAPK (unknown origin) | B | 7.7 | pIC50 | 19.95 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127412-127412 [PMID:32717614] |
ChEMBL | Inhibition of p38alpha-mediated TNFalpha secretion in LPS-stimulated human whole blood assessed as IC50 equals to free drug concentration at human whole blood IC50 | B | 7.76 | pIC50 | 17.38 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-3883 [PMID:22608965] |
ChEMBL | Inhibition of p38alpha kinase | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-3883 [PMID:22608965] |
ChEMBL | Inhibition of p38alpha kinase | B | 7.8 | pIC50 | 15.85 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-3883 [PMID:22608965] |
GtoPdb | - | - | 7.81 | pIC50 | 15.58 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3879-83 [PMID:22608965] |
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]