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Assay Detail

CHEMBL2383019

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of GST-fused human recombinant PI3Kalpha expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP
ChEMBL ↗
41
Total Activities
41
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Staben ST, Ndubaku C, Blaquiere N, Belvin M, Bull RJ, Dudley D, Edgar K, Gray D, Heald R, Heffron TP, Jones GE, Jones M, Kolesnikov A, Lee L, Lesnick J, Lewis C, Murray J, McLean NJ, Nonomiya J, Olivero AG, Ord R, Pang J, Price S, Prior WW, Rouge L, Salphati L, Sampath D, Wallin J, Wang L, Wei B, Weismann C, Wu P.
Bioorg Med Chem Lett (2013) 23 : 2606 -2613
PubMed 23540645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.09 8.89
Ki 17 9.56 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381382 — — 1 10.40
CHEMBL2381376 — — 1 10.22
CHEMBL2381375 — — 1 10.22
CHEMBL2381377 — — 1 9.96
CHEMBL2381380 — — 1 9.89
CHEMBL2381379 — — 1 9.85
CHEMBL2381374 — — 1 9.82
CHEMBL2381381 — — 1 9.74
CHEMBL2381378 — — 1 9.74
CHEMBL2381373 — — 1 9.57
CHEMBL2381279 — — 1 9.33
CHEMBL2381277 — — 1 9.21
CHEMBL2381275 — — 1 9.16
CHEMBL2381276 — — 1 9.05
CHEMBL2381278 — — 1 9.03
CHEMBL2381251 — — 1 8.89
CHEMBL2381271 — — 1 8.89
CHEMBL2381273 — — 1 8.85
CHEMBL2381266 — — 1 8.82
CHEMBL2381274 — — 1 8.72
CHEMBL2381270 — — 1 8.70
CHEMBL2381268 — — 1 8.70
CHEMBL2381261 — — 1 8.60
CHEMBL521851 PICTILISIB 2.0 1 8.59
CHEMBL2381253 — — 1 8.51
CHEMBL2381252 — — 1 8.48
CHEMBL2381254 — — 1 8.48
CHEMBL2381264 — — 1 8.46
CHEMBL2381255 — — 1 8.44
CHEMBL2322764 — — 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381382 — Ki = 0.04 nM 10.40
CHEMBL2381376 — Ki = 0.06 nM 10.22
CHEMBL2381375 — Ki = 0.06 nM 10.22
CHEMBL2381377 — Ki = 0.11 nM 9.96
CHEMBL2381380 — Ki = 0.13 nM 9.89
CHEMBL2381379 — Ki = 0.14 nM 9.85
CHEMBL2381374 — Ki = 0.15 nM 9.82
CHEMBL2381381 — Ki = 0.18 nM 9.74
CHEMBL2381378 — Ki = 0.18 nM 9.74
CHEMBL2381373 — Ki = 0.27 nM 9.57
CHEMBL2381279 — Ki = 0.47 nM 9.33
CHEMBL2381277 — Ki = 0.61 nM 9.21
CHEMBL2381275 — Ki = 0.69 nM 9.16
CHEMBL2381276 — Ki = 0.9 nM 9.05
CHEMBL2381278 — Ki = 0.94 nM 9.03
CHEMBL2381251 — IC50 = 1.3 nM 8.89
CHEMBL2381271 — IC50 = 1.3 nM 8.89
CHEMBL2381273 — IC50 = 1.4 nM 8.85
CHEMBL2381266 — IC50 = 1.5 nM 8.82
CHEMBL2381274 — Ki = 1.9 nM 8.72
CHEMBL2381270 — IC50 = 2.0 nM 8.70
CHEMBL2381268 — IC50 = 2.0 nM 8.70
CHEMBL2381261 — IC50 = 2.5 nM 8.60
CHEMBL521851 PICTILISIB Ki = 2.6 nM 8.59
CHEMBL2381253 — IC50 = 3.1 nM 8.51
CHEMBL2381252 — IC50 = 3.3 nM 8.48
CHEMBL2381254 — IC50 = 3.3 nM 8.48
CHEMBL2381264 — IC50 = 3.5 nM 8.46
CHEMBL2381255 — IC50 = 3.6 nM 8.44
CHEMBL2322764 — IC50 = 4.0 nM 8.40
CHEMBL2381267 — IC50 = 4.9 nM 8.31
CHEMBL2381262 — IC50 = 6.4 nM 8.19
CHEMBL2381263 — IC50 = 11.0 nM 7.96
CHEMBL2381272 — IC50 = 14.0 nM 7.85
CHEMBL2381258 — IC50 = 33.0 nM 7.48
CHEMBL2381256 — IC50 = 49.0 nM 7.31
CHEMBL2381257 — IC50 = 140.0 nM 6.85
CHEMBL2381260 — IC50 = 426.0 nM 6.37
CHEMBL2381259 — IC50 = 2900.0 nM 5.54
CHEMBL2381265 — IC50 < 0.5 nM -
CHEMBL2381269 — IC50 < 0.5 nM -