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Assay Detail

CHEMBL3413522

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

Binding
Inhibition of recombinant PI3Kalpha (unknown origin) using biotinylated PIP2 as substrate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
Pike KG, Morris J, Ruston L, Pass SL, Greenwood R, Williams EJ, Demeritt J, Culshaw JD, Gill K, Pass M, Finlay MR, Good CJ, Roberts CA, Currie GS, Blades K, Eden JM, Pearson SE.
J Med Chem (2015) 58 : 2326 -2349
PubMed 25643210 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.50 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030451 1 6.25
CHEMBL3410675 1 6.25
CHEMBL3410672 1 6.04
CHEMBL3410548 1 5.49
CHEMBL3410642 1 5.10
CHEMBL1312643 1 4.76
CHEMBL2030436 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030451 IC50 = 562.34 nM 6.25
CHEMBL3410675 IC50 = 562.34 nM 6.25
CHEMBL3410672 IC50 = 912.01 nM 6.04
CHEMBL3410548 IC50 = 3235.94 nM 5.49
CHEMBL3410642 IC50 = 7943.28 nM 5.10
CHEMBL1312643 IC50 = 17378.01 nM 4.76
CHEMBL2030436 IC50 = 26302.68 nM 4.58