rizavasertib [Ligand Id: 8204] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL379300 (A-443654, A-4436554) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of Akt1 in presence of 10 uM ATP | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3740-3744 [PMID:16678413] |
| ChEMBL | Inhibition of AKT1 | B | 9.8 | pKi | 0.16 | nM | Ki | Nat Chem Biol (2009) 5: 484-493 [PMID:19465931] |
| ChEMBL | Binding affinity to AKT1 (unknown origin) | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| GtoPdb | - | - | 9.8 | pKi | 0.16 | nM | Ki | Mol Cancer Ther (2005) 4: 977-86 [PMID:15956255] |
| ChEMBL | Inhibition of myristoylated wild type AKT1 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Nat Chem Biol (2009) 5: 484-493 [PMID:19465931] |
| ChEMBL | Inhibition of human Akt1 | B | 9.8 | pIC50 | 0.16 | nM | IC50 | J Med Chem (2007) 50: 2990-3003 [PMID:17523610] |
| ChEMBL | Inhibition of Akt | B | 9.8 | pIC50 | 0.16 | nM | IC50 | Eur J Med Chem (2009) 44: 4090-4097 [PMID:19497644] |
| AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| GtoPdb | - | - | 9.8 | pKi | ~0.16 | nM | Ki | Mol Cancer Ther (2005) 4: 977-86 [PMID:15956255] |
| ChEMBL | Inhibition of myristoylated wild type AKT2 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Nat Chem Biol (2009) 5: 484-493 [PMID:19465931] |
| AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| GtoPdb | - | - | 9.8 | pKi | ~0.16 | nM | Ki | Mol Cancer Ther (2005) 4: 977-86 [PMID:15956255] |
| ChEMBL | Inhibition of myristoylated wild type AKT3 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay | B | 7.29 | pIC50 | 51 | nM | IC50 | Nat Chem Biol (2009) 5: 484-493 [PMID:19465931] |
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]
