ChEMBL ligand: CHEMBL3683575 (Ioa 244, IOA-244, IOA244, Msc-2360844, MSC2360844)

phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 2/phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/phosphoinositide-3-kinase regulatory subunit 5/phosphoinositide-3-kinase regulatory subunit 3/PI3-kinase class I in Human [ChEMBL: CHEMBL3559703] [GtoPdb: 2155, 2504, 2503, 2153, 2154, 2156, 2506, 2505] [UniProtKB: O00329, O00459, P27986, P42336, P42338, P48736, Q8WYR1, Q92569] 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 delta/phosphoinositide-3-kinase regulatory subunit 2/phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/phosphoinositide-3-kinase regulatory subunit 5/phosphoinositide-3-kinase regulatory subunit 3/PI3-kinase class I in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL3559703] [GtoPdb: 2155, 2504, 2503, 2153, 2154, 2156, 2506, 2505] [UniProtKB: O00329, O00459, P27986, P42336, P42338, P48736, Q8WYR1, Q92569]
ChEMBL	Binding Assay: The efficacy of compounds of the invention in inhibiting the PI3K induced-lipid phosphorylation may be tested in the following binding assay. The assay combines the scintillation proximity assay technology (SPA, Amersham) with the capacity of neomycin (a polycationic antibiotic) to bind phospholipids with high affinity and specificity. The Scintillation Proximity Assay is based on the properties of weakly emitting isotopes (such as 3H, 125I, 33P). Coating SPA beads with neomycin allows the detection of phosphorylated lipid substrates after incubation with recombinant PI3K and radioactive ATP in the same well, by capturing the radioactive phospholipids to the SPA beads through their specific binding to neomycin. To a 384 wells MTP containing 5 ul of the test compound of Formula (I) (solubilized in 2% DMSO; to yield a final concentration of 20, 5, 1.25, 0.3125, 0.0781, 0.0195, 0.0049, 0.0012, 0.0003 and 0.00075 uM of the test compound).	B	6.46	pIC50	347	nM	IC50	US-9073940-B2. Tricyclic pyrazol amine derivatives (2015)
GtoPdb	Inhibitory efficacy determined by Scintillation Proximity Assay detecting phosphorylated lipid substrates after incubation with recombinant PI3Kδ and radioactive ATP.	-	6.46	pIC50	347	nM	IC50	US9073940B2. Tricyclic pyrazol amine derivatives (2015)

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]