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Assay Detail

CHEMBL4713357

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Functional
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
14
Total Activities
14
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

Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR inhibitors.
Li J,An B,Song X,Zhang Q,Chen C,Wei S,Fan R,Li X,Zou Y
Eur J Med Chem (2021) 212 : 113019 -113019
PubMed 33429247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 9.64 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353410 OSIMERTINIB 4.0 1 10.96
CHEMBL4793880 1 10.68
CHEMBL4760063 1 10.13
CHEMBL4758350 1 9.48
CHEMBL4787215 1 9.39
CHEMBL4749234 1 9.35
CHEMBL4748458 1 9.27
CHEMBL4752548 1 9.26
CHEMBL4747980 1 8.95
CHEMBL4796376 1 8.89
CHEMBL4781323 1 -
CHEMBL4796010 1 -
CHEMBL4781799 1 -
CHEMBL4747082 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353410 OSIMERTINIB IC50 = 0.011 nM 10.96
CHEMBL4793880 IC50 = 0.021 nM 10.68
CHEMBL4760063 IC50 = 0.074 nM 10.13
CHEMBL4758350 IC50 = 0.333 nM 9.48
CHEMBL4787215 IC50 = 0.411 nM 9.39
CHEMBL4749234 IC50 = 0.445 nM 9.35
CHEMBL4748458 IC50 = 0.543 nM 9.27
CHEMBL4752548 IC50 = 0.544 nM 9.26
CHEMBL4747980 IC50 = 1.12 nM 8.95
CHEMBL4796376 IC50 = 1.301 nM 8.89
CHEMBL4781323 IC50 = 0.008 nM -
CHEMBL4796010 IC50 = 0.008 nM -
CHEMBL4781799 IC50 = 0.008 nM -
CHEMBL4747082 IC50 = 0.009 nM -