ChEMBL ligand: CHEMBL2387080 (GDC-0032, RG-7604, Taselisib)
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!
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-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443] 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!
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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL	Inhibition of DNA-dependent protein kinase (unknown origin)	B	5.32	pIC50	>4800	nM	IC50	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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	Inhibition of human VPS34	B	6.43	pIC50	374	nM	IC50	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Selectivity interaction (Enzymatic assay) EUB0000685a PIK3C3	B	6.43	pIC50	374	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
ChEMBL	Inhibition of PI3KC2beta (unknown origin)	B	6.53	pIC50	292	nM	IC50	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Selectivity interaction (Enzymatic assay) EUB0000685a PIK3C2B	B	6.53	pIC50	292	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
ChEMBL	Inhibition of PI3KC2alpha (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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 recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assay	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2016) 59: 985-1002 [PMID:26741947]
ChEMBL	Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assay	B	9.54	pKi	0.29	nM	Ki	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Affinity Biochemical interaction (Enzymatic fluorescence polarization assay) EUB0000685a PIK3CA	B	9.54	pKi	0.29	nM	Ki	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb	-	-	9.54	pKi	0.29	nM	Ki	J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL	Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assay	B	10.05	pKi	0.09	nM	Ki	J Med Chem (2022) 65: 16589-16621 [PMID:36455032]
GtoPdb	-	-	10.05	pKi	0.09	nM	Ki	US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
ChEMBL	Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation	B	7.51	pIC50	31	nM	IC50	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Inhibition of PI3Kalpha in human MCF7-neo/Her2 cells assessed as reduction of AKT phosphorylation at S473	B	8.4	pIC50	4	nM	IC50	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Affinity Phenotypic Cellular interaction (MesoScale Discovery assay (AKT phoshorylation in MCF 7 cells)) EUB0000685a PIK3CA	B	8.4	pIC50	4	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of PI3K alpha (unknown origin)	B	9.15	pIC50	<0.7	nM	IC50	ACS Med Chem Lett (2017) 8: 808-813 [PMID:28835793]
ChEMBL	Inhibition of PI3Kalpha H1047R mutant in human HCC1954 cells assessed as reduction in PRAS40 phosphorylation after 24 hrs by electrochemiluminescent assay	B	7.62	pEC50	24	nM	EC50	J Med Chem (2022) 65: 16589-16621 [PMID:36455032]
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	-	-	7.28	pKi	53	nM	Ki	US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
GtoPdb	-	-	8.04	pKi	9.1	nM	Ki	J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL	Inhibition of PI3Kbeta (unknown origin)	B	8.04	pKi	9.1	nM	Ki	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Affinity Biochemical interaction (Enzymatic fluorescence polarization assay) EUB0000685a PIK3CB	B	8.04	pKi	9.1	nM	Ki	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Affinity Phenotypic Cellular interaction (MesoScale Discovery assay (AKT phoshorylation in MCF 7 cells)) EUB0000685a PIK3CB	B	8.4	pIC50	4	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
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	-	-	9.68	pKi	0.21	nM	Ki	J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL	Inhibition of PI3Kdelta (unknown origin)	B	9.92	pKi	0.12	nM	Ki	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Affinity Biochemical interaction (Enzymatic fluorescence polarization assay) EUB0000685a PIK3CD	B	9.92	pKi	0.12	nM	Ki	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb	-	-	10.1	pKi	0.08	nM	Ki	US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
ChEMBL	Affinity Phenotypic Cellular interaction (MesoScale Discovery assay (AKT phoshorylation in MCF 7 cells)) EUB0000685a PIK3CD	B	8.4	pIC50	4	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of PI3K delta (unknown origin)	B	9.15	pIC50	<0.7	nM	IC50	ACS Med Chem Lett (2017) 8: 808-813 [PMID:28835793]
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]
GtoPdb	-	-	8.84	pKi	1.43	nM	Ki	US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
GtoPdb	-	-	9.01	pKi	0.97	nM	Ki	J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL	Inhibition of PI3Kgamma (unknown origin)	B	9.01	pKi	0.97	nM	Ki	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL	Affinity Biochemical interaction (Enzymatic fluorescence polarization assay) EUB0000685a PIK3CG	B	9.01	pKi	0.97	nM	Ki	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Affinity Phenotypic Cellular interaction (MesoScale Discovery assay (AKT phoshorylation in MCF 7 cells)) EUB0000685a PIK3CG	B	8.4	pIC50	4	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
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 (unknown origin)	B	5.92	pKi	1200	nM	Ki	J Med Chem (2013) 56: 4597-4610 [PMID:23662903]

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]