CP466722 [Ligand Id: 9359] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL2143829 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 (unknown origin) using p53-based peptide substrate preincubated for 5 min prior to ATP addition | B | 6.06 | pIC50 | 879 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
| 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 | 5.83 | pIC50 | 1490 | 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 | 5.26 | pIC50 | 5440 | 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 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 | 5.47 | pIC50 | 3420 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
| ChEMBL | Inhibition of ATM in human MCF7 cells assessed as reduction in KAP1 phosphorylation | B | 6.32 | pIC50 | 480 | nM | IC50 | J Med Chem (2019) 62: 2988-3008 [PMID:30840447] |
| ChEMBL | Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2016) 59: 559-577 [PMID:26632965] |
| 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 | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
| ChEMBL | Inhibition of flag-tagged ATM (unknown origin) using p53 as substrate by ELISA | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2016) 59: 559-577 [PMID:26632965] |
| ChEMBL | Inhibition of full length Flag-tagged ATM (unknown origin) using GST-p53(1 to 101 residues) as substrates incubated for 90 mins | B | 7.89 | pIC50 | 12.9 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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 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 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 | 5.34 | pIC50 | 4590 | nM | IC50 | J Med Chem (2016) 59: 6281-6292 [PMID:27259031] |
ChEMBL data shown on this page come from version 33:
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]
