ChEMBL ligand: CHEMBL2216859 (GSK-2269557, GSK-2269557A, GSK2269557A, GSK-2269557 FREE BASE, Nemiralisib)
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!
Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809] 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
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	In a homogeneous time-resolved fluorescence (HTRF) assay	-	5.3	pIC50	5011	nM	IC50	J Med Chem (2015) 58: 7381-99 [PMID:26301626]
ChEMBL	Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method	B	5.3	pIC50	5011.87	nM	IC50	J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
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	In a homogeneous time-resolved fluorescence (HTRF) assay	-	5.8	pIC50	1584	nM	IC50	J Med Chem (2015) 58: 7381-99 [PMID:26301626]
ChEMBL	Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method	B	5.8	pIC50	1584.89	nM	IC50	J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
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]
ChEMBL	Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method	B	9.9	pKi	0.13	nM	Ki	J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
ChEMBL	Inhibition of PI3Kdelta	B	7	pIC50	<100	nM	IC50	J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
GtoPdb	In a homogeneous time-resolved fluorescence (HTRF) assay in the presence of 2mM ATP.	-	9.9	pIC50	0.13	nM	IC50	J Med Chem (2015) 58: 7381-99 [PMID:26301626]
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	In a homogeneous time-resolved fluorescence (HTRF) assay	-	5.2	pIC50	6310	nM	IC50	J Med Chem (2015) 58: 7381-99 [PMID:26301626]
ChEMBL	Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method	B	5.2	pIC50	6309.57	nM	IC50	J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
GtoPdb	-	-	5.5	pIC50	3162	nM	IC50	J Med Chem (2015) 58: 7381-99 [PMID:26301626]

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]