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 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]