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Assay Detail

CHEMBL4712543

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

Binding
Inhibition of PI3K p110alpha H1047R mutant in human T47D cells assessed as reduction in phosphorylation of Akt at T308 residue incubated for 2 hrs by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T47D
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
Cheng H,Orr STM,Bailey S,Brooun A,Chen P,Deal JG,Deng YL,Edwards MP,Gallego GM,Grodsky N,Huang B,Jalaie M,Kaiser S,Kania RS,Kephart SE,Lafontaine J,Ornelas MA,Pairish M,Planken S,Shen H,Sutton S,Zehnder L,Almaden CD,Bagrodia S,Falk MD,Gukasyan HJ,Ho C,Kang X,Kosa RE,Liu L,Spilker ME,Timofeevski S,Visswanathan R,Wang Z,Meng F,Ren S,Shao L,Xu F,Kath JC
J Med Chem (2021) 64 : 644 -661
PubMed 33356246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.79 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756555 1 8.06
CHEMBL2396661 ALPELISIB 4.0 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756555 IC50 = 8.7 nM 8.06
CHEMBL2396661 ALPELISIB IC50 = 30.0 nM 7.52