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Assay Detail

CHEMBL5529685

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

Binding
Inhibition of PI3Kalpha in human BT-474 cells incubated for 140 mins by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BT-474
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG, Hunt TA, Barlaam B, Benstead D, Cadogan E, Chen K, Cook CR, Colclough N, Deng C, Durant ST, Eatherton A, Goldberg K, Johnström P, Liu L, Liu Z, Nissink JWM, Pang C, Pass M, Robb GR, Roberts C, Schou M, Steward O, Sykes A, Yan Y, Zhai B, Zheng L.
J Med Chem (2024) 67 : 3090 -3111
PubMed 38306388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.80 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555756 1 6.50
CHEMBL3960662 1 6.20
CHEMBL5572255 1 5.70
CHEMBL5566946 1 4.80
CHEMBL5575600 1 -
CHEMBL4594429 AZD-1390 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555756 IC50 = 316.23 nM 6.50
CHEMBL3960662 IC50 = 630.96 nM 6.20
CHEMBL5572255 IC50 = 1995.26 nM 5.70
CHEMBL5566946 IC50 = 15848.93 nM 4.80
CHEMBL5575600 IC50 > 5011.87 nM -
CHEMBL4594429 AZD-1390 IC50 > 12589.25 nM -