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Assay Detail

CHEMBL4146245

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

Functional
Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.
Geng K, Xia Z, Ji Y, Zhang RR, Sun D, Ai J, Song Z, Geng M, Zhang A.
Eur J Med Chem (2018) 144 : 386 -397
PubMed 29288940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.14 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168868 1 9.70
CHEMBL3286830 LORLATINIB 4.0 1 8.92
CHEMBL601719 CRIZOTINIB 4.0 1 7.31
CHEMBL2403108 CERITINIB 4.0 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168868 IC50 = 0.2 nM 9.70
CHEMBL3286830 LORLATINIB IC50 = 1.2 nM 8.92
CHEMBL601719 CRIZOTINIB IC50 = 48.6 nM 7.31
CHEMBL2403108 CERITINIB IC50 = 234.0 nM 6.63