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Assay Detail

CHEMBL5389547

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

Functional
Cytotoxicity against human T47D cells harboring PI3Kalpha H1047R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 luminescent cell viability assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T47D
Confidence 1 — Organism
Curated By Autocuration

Target

T47D (CHEMBL614361)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
Ketcham JM, Harwood SJ, Aranda R, Aloiau AN, Bobek BM, Briere DM, Burns AC, Caddell Haatveit K, Calinisan A, Clarine J, Elliott A, Engstrom LD, Gunn RJ, Ivetac A, Jones B, Kuehler J, Lawson JD, Nguyen N, Parker C, Pearson KE, Rahbaek L, Saechao B, Wang X, Waters A, Waters L, Watkins AH, Olson P, Smith CR, Christensen JG, Marx MA.
J Med Chem (2024) 67 : 4936 -4949
PubMed 38477582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.55 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5402470 1 7.32
CHEMBL5437679 1 7.25
CHEMBL5424195 1 7.15
CHEMBL5414256 1 7.07
CHEMBL5423227 1 6.92
CHEMBL5411976 1 6.87
CHEMBL5406950 1 6.82
CHEMBL5419204 1 6.80
CHEMBL5406570 1 6.74
CHEMBL5408522 1 6.61
CHEMBL5430524 1 6.52
CHEMBL5404456 1 6.31
CHEMBL5424291 1 6.25
CHEMBL5422741 1 6.20
CHEMBL5436038 1 5.96
CHEMBL5409207 1 5.43
CHEMBL5440814 1 5.21
CHEMBL5401780 1 -
CHEMBL5413908 1 -
CHEMBL5431134 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5402470 IC50 = 48.0 nM 7.32
CHEMBL5437679 IC50 = 56.0 nM 7.25
CHEMBL5424195 IC50 = 71.0 nM 7.15
CHEMBL5414256 IC50 = 86.0 nM 7.07
CHEMBL5423227 IC50 = 120.0 nM 6.92
CHEMBL5411976 IC50 = 135.0 nM 6.87
CHEMBL5406950 IC50 = 151.0 nM 6.82
CHEMBL5419204 IC50 = 160.0 nM 6.80
CHEMBL5406570 IC50 = 183.0 nM 6.74
CHEMBL5408522 IC50 = 246.0 nM 6.61
CHEMBL5430524 IC50 = 304.0 nM 6.52
CHEMBL5404456 IC50 = 488.0 nM 6.31
CHEMBL5424291 IC50 = 566.0 nM 6.25
CHEMBL5422741 IC50 = 627.0 nM 6.20
CHEMBL5436038 IC50 = 1110.0 nM 5.96
CHEMBL5409207 IC50 = 3725.0 nM 5.43
CHEMBL5440814 IC50 = 6239.0 nM 5.21
CHEMBL5401780 IC50 > 10000.0 nM -
CHEMBL5413908 IC50 > 10000.0 nM -
CHEMBL5431134 IC50 > 10000.0 nM -