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Assay Detail

CHEMBL4398835

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Functional
Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR<sup>L858R/T790M/C797S</sup>.
Li Q, Zhang T, Li S, Tong L, Li J, Su Z, Feng F, Sun D, Tong Y, Wang X, Zhao Z, Zhu L, Ding J, Li H, Xie H, Xu Y.
ACS Med Chem Lett (2019) 10 : 869 -873
PubMed 31223440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.99 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545311 BRIGATINIB 4.0 1 6.38
CHEMBL4443483 1 6.19
CHEMBL3353410 OSIMERTINIB 4.0 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545311 BRIGATINIB IC50 = 420.0 nM 6.38
CHEMBL4443483 IC50 = 640.0 nM 6.19
CHEMBL3353410 OSIMERTINIB IC50 = 3930.0 nM 5.41