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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 34:
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]