ChEMBL ligand: CHEMBL1081312
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] There should be some charts here, you may need to enable JavaScript!
EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit 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/PI3-kinase p110-beta subunit 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 delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] There should be some charts here, you may need to enable JavaScript!
ATR serine/threonine kinase/Serine-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!
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] There should be some charts here, you may need to enable JavaScript!
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234] 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]
GtoPdb	-	-	7.22	pIC50	60	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of DNA-PK by radioactive phosphotransfer assay in presence of 10 uM ATP	B	7.22	pIC50	60	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL	Inhibition of recombinant EphB4R by radioactive phosphotransfer assay in presence of 10 uM ATP	B	6.72	pIC50	190	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL	Inhibition of recombinant EGFR by radioactive phosphotransfer assay in presence of 10 uM ATP	B	6.59	pIC50	260	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of EGFR (unknown origin)	B	6.59	pIC50	260	nM	IC50	Medchemcomm (2012) 3: 1337-1355
GtoPdb	-	-	6.59	pIC50	260	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
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]
GtoPdb	-	-	7.28	pIC50	52	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of PI3K p110-alpha	B	7.28	pIC50	52	nM	IC50	J Med Chem (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL	Inhibition of recombinant PI3Kalpha by radioactive phosphotransfer assay in presence of 10 uM ATP	B	7.28	pIC50	52	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of PI3Kalpha (unknown origin)	B	7.28	pIC50	52	nM	IC50	Medchemcomm (2012) 3: 1337-1355
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]
GtoPdb	-	-	5.85	pIC50	1400	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of recombinant PI3Kbeta by radioactive phosphotransfer assay in presence of 10 uM ATP	B	5.85	pIC50	1400	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of PI3Kbeta (unknown origin)	B	5.85	pIC50	1400	nM	IC50	Medchemcomm (2012) 3: 1337-1355
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
GtoPdb	-	-	6.82	pIC50	150	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of recombinant PI3Kdelta by radioactive phosphotransfer assay in presence of 10 uM ATP	B	6.82	pIC50	150	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of PI3Kdelta (unknown origin)	B	6.82	pIC50	150	nM	IC50	Medchemcomm (2012) 3: 1337-1355
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 recombinant PI3Kgamma by radioactive phosphotransfer assay in presence of 10 uM ATP	B	5.96	pIC50	1100	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of PI3Kgamma (unknown origin)	B	5.96	pIC50	1100	nM	IC50	Medchemcomm (2012) 3: 1337-1355
GtoPdb	-	-	5.96	pIC50	1100	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL	Inhibition of recombinant PI4Kbeta by radioactive phosphotransfer assay in presence of 10 uM ATP	B	7.22	pIC50	60	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL	Inhibition of human recombinant FLAG-tagged full length ATR expressed in mammalian cell line co-expressing human recombinant cMyc-tagged full length ATRIP	B	5.85	pIC50	1420	nM	IC50	Bioorg Med Chem Lett (2017) 27: 750-754 [PMID:28131712]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
GtoPdb	-	-	8	pIC50	10	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of mTOR	B	8	pIC50	10	nM	IC50	J Med Chem (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL	Inhibition of recombinant mTOR by radioactive phosphotransfer assay in presence of 10 uM ATP	B	8	pIC50	<10	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of mTOR (unknown origin)	B	8	pIC50	10	nM	IC50	Medchemcomm (2012) 3: 1337-1355
ChEMBL	Inhibition of mTOR (unknown origin) using U-Light-4E-BP1 peptide as a substrate in the presence of ATP incubated for 30 mins by Lance ultra assay	B	8	pIC50	10	nM	IC50	Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167]
ChEMBL	Inhibition of recombinant mTOR (unknown origin) using 4EBP1 as substrate in presence of [gamma-32P]ATP by radiometric scintillation assay	B	8	pIC50	10	nM	IC50	Eur J Med Chem (2020) 208: 112820-112820 [PMID:32966896]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
GtoPdb	-	-	7.74	pIC50	18	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of recombinant c-Abl by radioactive phosphotransfer assay in presence of 10 uM ATP	B	7.74	pIC50	18	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of ABL (unknown origin)	B	7.74	pIC50	18	nM	IC50	Medchemcomm (2012) 3: 1337-1355
ChEMBL	Inhibition of ABL1 at 1 uM after 60 mins by FRET assay in presence of 10 uM ATP	B	8.7	pIC50	2	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL	Inhibition of recombinant HCK by radioactive phosphotransfer assay in presence of 10 uM ATP	B	8.1	pIC50	8	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of HCK (unknown origin)	B	8.1	pIC50	8	nM	IC50	Medchemcomm (2012) 3: 1337-1355
GtoPdb	-	-	8.1	pIC50	8	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL	Inhibition of Ret	B	9	pIC50	<1	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
GtoPdb	-	-	7.85	pIC50	14	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of Src	B	7.85	pIC50	14	nM	IC50	J Med Chem (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL	Inhibition of recombinant c-Src by radioactive phosphotransfer assay in presence of 10 uM ATP	B	7.85	pIC50	14	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
ChEMBL	Inhibition of Src (unknown origin)	B	7.85	pIC50	14	nM	IC50	Medchemcomm (2012) 3: 1337-1355
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL	Inhibition of VEGFR2-mediated proliferation of HUVEC in VEGF-supplemented medium at 0.04 to 10 uM after 24 hrs by fluorescence assay	B	7.39	pIC50	41	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
GtoPdb	-	-	7.92	pIC50	12	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL	Inhibition of VEGFR2	B	7.92	pIC50	12	nM	IC50	J Med Chem (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL	Inhibition of recombinant VEGFR2 by radioactive phosphotransfer assay in presence of 10 uM ATP	B	7.92	pIC50	12	nM	IC50	Nat Chem Biol (2008) 4: 691-699 [PMID:18849971]
platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
GtoPdb	-	-	8.7	pIC50	2	nM	IC50	Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]

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]