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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 | 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 | 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 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 32:
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]