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Assay Detail

CHEMBL5035304

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

Functional
Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT 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 Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.
Liu Z, Yu P, Dong L, Wang W, Duan S, Wang B, Gong X, Ye L, Wang H, Tian J.
J Med Chem (2021) 64 : 10286 -10296
PubMed 34253025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.45 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5093999 1 9.40
CHEMBL4297627 SELITRECTINIB 2.0 1 8.17
CHEMBL5080010 1 8.11
CHEMBL4298138 REPOTRECTINIB 4.0 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5093999 IC50 = 0.4 nM 9.40
CHEMBL4297627 SELITRECTINIB IC50 = 6.8 nM 8.17
CHEMBL5080010 IC50 = 7.7 nM 8.11
CHEMBL4298138 REPOTRECTINIB IC50 = 8.0 nM 8.10