ChEMBL ligand: CHEMBL2140173
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] There should be some charts here, you may need to enable JavaScript!
ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] There should be some charts here, you may need to enable JavaScript!
ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] There should be some charts here, you may need to enable JavaScript!
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] 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 catalytic subunit 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	6.69	pIC50	204	nM	IC50	J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
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]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 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	452	nM	IC50	J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 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	5.67	pIC50	2140	nM	IC50	J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 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	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	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	6.83	pIC50	149	nM	IC50	J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
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 (unknown origin)	B	8.2	pIC50	6.3	nM	IC50	J Med Chem (2020) 63: 14151-14183 [PMID:33135887]
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]
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	9.1	pIC50	0.8	nM	IC50	J Med Chem (2016) 59: 6281-6292 [PMID:27259031]
ATR checkpoint kinase/Serine/threonine-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	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	5.07	pIC50	8500	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	5.18	pIC50	6550	nM	IC50	J Med Chem (2016) 59: 6281-6292 [PMID:27259031]

ChEMBL data shown on this page come from version 36:

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]