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ChEMBL ligand: CHEMBL2140173 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
ChEMBL | Inhibition of DNA-PK isolated from human HeLa cells assessed as reduction in p53 Ser15 phosphorylation by HTRF assay | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
ChEMBL | Binding affinity to human Vps34 expressed in mammalian expression system | B | 8.77 | pKd | 1.7 | nM | Kd | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
ChEMBL | Binding affinity to Vps34 (unknown origin) | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2022) 65: 15993-16032 [PMID:36490325] |
ChEMBL | Inhibition of recombinant full-length human VPS34 incubated for 60 mins by ADP-Glo kinase assay | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
ChEMBL | Binding affinity to ATM (unknown origin) | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2022) 65: 15993-16032 [PMID:36490325] |
ChEMBL | Inhibition of ATM in human MCF7 cells assessed as reduction in etoposide-stimulated KAP1 phosphorylation incubated for 1 hr by ICW assay | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
ChEMBL | Inhibition of ATM (unknown origin) | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2022) 65: 15993-16032 [PMID:36490325] |
ChEMBL | Competitive inhibition of ATM (unknown origin) measured by ATP-competitive binding assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2022) 233: 114196-114196 [PMID:35231830] |
ChEMBL | Inhibition of recombinant full-length human FLAG-tagged ATM assessed as reduction in p53 S15 phosphorylation incubated for 30 mins by ELISA | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
GtoPdb | - | - | 8.2 | pIC50 | 6.3 | nM | IC50 | Mol Cancer Ther (2009) 8: 2894-902 [PMID:19808981] |
ChEMBL | Inhibition of ATM kinase in human glioma cells | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2015) 58: 41-71 [PMID:25387153] |
ChEMBL | Inhibition of ATM (unknown origin) by biochemical assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
ChEMBL | Inhibition of ATR in human HeLa cells incubated for 4 hrs | B | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
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]