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Assay Detail

CHEMBL5161053

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Functional
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR T790M/L858R mutant by sulforhodamine B assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1975
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1975 (CHEMBL614348)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.
Tang Q, Peng T, Hu J, Zhang T, Chen P, Chen D, Wang Y, Chen L, Tong L, Chen Y, Xie H, Liang G.
Eur J Med Chem (2022) 233 : 114249 -114249
PubMed 35259690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.91 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5182791 1 5.46
CHEMBL5208907 1 5.23
CHEMBL5198424 1 5.01
CHEMBL5194966 1 4.96
CHEMBL5174372 1 4.86
CHEMBL5193902 1 4.82
CHEMBL5169328 1 4.77
CHEMBL5200760 1 4.74
CHEMBL5176588 1 4.65
CHEMBL5180251 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5182791 IC50 = 3500.0 nM 5.46
CHEMBL5208907 IC50 = 5900.0 nM 5.23
CHEMBL5198424 IC50 = 9820.0 nM 5.01
CHEMBL5194966 IC50 = 10850.0 nM 4.96
CHEMBL5174372 IC50 = 13890.0 nM 4.86
CHEMBL5193902 IC50 = 15020.0 nM 4.82
CHEMBL5169328 IC50 = 16880.0 nM 4.77
CHEMBL5200760 IC50 = 18130.0 nM 4.74
CHEMBL5176588 IC50 = 22590.0 nM 4.65
CHEMBL5180251 IC50 = 27220.0 nM 4.57