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Assay Detail

CHEMBL4829468

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

Functional
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
8
Total Activities
8
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

The synthesis and bioactivity of pyrrolo[2,3-d]pyrimidine derivatives as tyrosine kinase inhibitors for NSCLC cells with EGFR mutations.
Xia Z, Huang R, Zhou X, Chai Y, Chen H, Ma L, Yu Q, Li Y, Li W, He Y.
Eur J Med Chem (2021) 224 : 113711 -113711
PubMed 34315040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.20 5.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297865 ABIVERTINIB 3.0 1 5.81
CHEMBL4862044 1 5.78
CHEMBL4850239 1 5.51
CHEMBL4847264 1 5.42
CHEMBL4873503 1 5.38
CHEMBL3787662 1 4.66
CHEMBL4860999 1 4.65
CHEMBL4846913 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297865 ABIVERTINIB IC50 = 1560.0 nM 5.81
CHEMBL4862044 IC50 = 1670.0 nM 5.78
CHEMBL4850239 IC50 = 3100.0 nM 5.51
CHEMBL4847264 IC50 = 3840.0 nM 5.42
CHEMBL4873503 IC50 = 4120.0 nM 5.38
CHEMBL3787662 IC50 = 21980.0 nM 4.66
CHEMBL4860999 IC50 = 22430.0 nM 4.65
CHEMBL4846913 IC50 = 41980.0 nM 4.38