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ChEMBL ligand: CHEMBL222102 (KU-55933) |
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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 DNAPK after 2 hrs by radiometric phosphate incorporation assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2011) 54: 2320-2330 [PMID:21413798] |
ChEMBL | Inhibition of DNA-PK in HeLa cell nuclear extracts | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2007) 50: 1958-1972 [PMID:17371003] |
ChEMBL | Inhibition of DNAPK (unknown origin) using p53-based peptide substrate preincubated for 5 min prior to ATP addition | B | 6.74 | pIC50 | 183 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 5.32 | pIC50 | 4798 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
ChEMBL | Inhibition of human recombinant PI3Kalpha using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay | B | 6.34 | pIC50 | 458 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
ChEMBL | Inhibition of human recombinant PI3Kbeta using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay | B | 6.88 | pIC50 | 133 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
ChEMBL | Inhibition of human recombinant PI3Kgamma using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
ChEMBL | Inhibition of ATM | B | 8.66 | pKi | 2.2 | nM | Ki | Chem Biol (2005) 12: 621-637 [PMID:15975507] |
GtoPdb | - | - | 8.66 | pKi | 2.2 | nM | Ki | Cancer Res (2004) 64: 9152-9 [PMID:15604286] |
ChEMBL | Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis | B | 5.91 | pIC50 | 1220 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
ChEMBL | Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2016) 59: 559-577 [PMID:26632965] |
ChEMBL | Competitive inhibition of ATM (unknown origin) measured by ATP-competitive binding assay | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2022) 233: 114196-114196 [PMID:35231830] |
ChEMBL | Inhibition of ATM in human U2OS cells assessed as inhibition of p53 phosphorylation at Ser15 residue | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2016) 59: 559-577 [PMID:26632965] |
ChEMBL | Inhibition of ATM isolated from human HeLa cell extract using glutathione S-transferase-p53N66 as substrate by ELISA | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5352-5359 [PMID:22835870] |
ChEMBL | Inhibition of ATM (unknown origin) by ELISA method | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2023) 66: 9495-9518 [PMID:37438997] |
ChEMBL | Inhibition of full length recombinant ATM after 24 hrs by radiometric phosphate incorporation assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2011) 54: 2320-2330 [PMID:21413798] |
ChEMBL | Inhibition of human ATM using p53 as substrate preincubated for 10 mins by ELISA | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2016) 59: 559-577 [PMID:26632965] |
ChEMBL | Inhibition of ATM (unknown origin) by biochemical assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
ChEMBL | Inhibition of ATM kinase | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2007) 50: 1958-1972 [PMID:17371003] |
ChEMBL | Inhibition of human HeLa nuclear extract derived ATM using glutathioneS-transferase-p53N66 as substrate preincubated for 10 mins followed by ATP addition and measured after 1 hr by ELISA | B | 7.89 | pIC50 | 12.9 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
GtoPdb | - | - | 7.89 | pIC50 | 13 | nM | IC50 | Cancer Res (2004) 64: 9152-9 [PMID:15604286] |
ChEMBL | Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of ATP by HTRF method | B | 8.7 | pIC50 | <2 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
ChEMBL | Inhibition of full length recombinant ATR after 24 hrs by radiometric phosphate incorporation assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2011) 54: 2320-2330 [PMID:21413798] |
ChEMBL | Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
ChEMBL | Inhibition of mTOR by radiometric phosphate incorporation assay | B | 5.03 | pIC50 | 9300 | nM | IC50 | J Med Chem (2011) 54: 2320-2330 [PMID:21413798] |
ChEMBL | Inhibition of C-terminal FLAG-tagged recombinant mTOR (1362 to 2549 residues) (unknown origin) using Biotin-Ahx-Lys-Lys-Ala-Asn-Gln-Val-Phe-Leu-Gly-Phe-Thr-Tyr-Val-Ala-Pro-Ser-Val-Leu-Glu-Ser-Val-Lys-Glu-NH2 as substrate after 90 mins by AlphaScreen assay | B | 5.25 | pIC50 | 5580 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
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]