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Assay Detail

CHEMBL5711665

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

Functional
Cytotoxicity against mouse Ba/F3 EGFR-T790M/L858R cells assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Ba/F3 EGFR-T790M/L858R
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer.
Uchibori K, Inase N, Araki M, Kamada M, Sato S, Okuno Y, Fujita N, Katayama R.
Nat Commun (2017) 8 : 14768 -14768
PubMed 28287083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.88 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353410 OSIMERTINIB 4.0 1 8.39
CHEMBL3787344 NAZARTINIB 2.0 1 7.81
CHEMBL3397300 1 7.44
CHEMBL1173655 AFATINIB 4.0 1 7.41
CHEMBL3545311 BRIGATINIB 4.0 1 7.27
CHEMBL4203266 1 6.73
CHEMBL509032 TAE-684 1 6.63
CHEMBL2403108 CERITINIB 4.0 1 6.16
CHEMBL3545360 ASP-3026 1.0 1 5.77
CHEMBL939 GEFITINIB 4.0 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353410 OSIMERTINIB IC50 = 4.1 nM 8.39
CHEMBL3787344 NAZARTINIB IC50 = 15.5 nM 7.81
CHEMBL3397300 IC50 = 36.0 nM 7.44
CHEMBL1173655 AFATINIB IC50 = 39.2 nM 7.41
CHEMBL3545311 BRIGATINIB IC50 = 53.7 nM 7.27
CHEMBL4203266 IC50 = 184.5 nM 6.73
CHEMBL509032 TAE-684 IC50 = 232.6 nM 6.63
CHEMBL2403108 CERITINIB IC50 = 685.2 nM 6.16
CHEMBL3545360 ASP-3026 IC50 = 1691.0 nM 5.77
CHEMBL939 GEFITINIB IC50 = 5922.0 nM 5.23