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Assay Detail

CHEMBL5139776

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Functional
Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
5
Total Activities
5
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 quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.
Wu T, Qin Q, Lv R, Liu N, Yin W, Hao C, Sun Y, Zhang C, Sun Y, Zhao D, Cheng M.
Eur J Med Chem (2022) 238 : 114451 -114451
PubMed 35617855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.57 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297627 SELITRECTINIB 2.0 1 8.09
CHEMBL5175892 1 7.80
CHEMBL5206613 1 7.70
CHEMBL457614 1 7.70
CHEMBL4856292 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297627 SELITRECTINIB IC50 = 8.2 nM 8.09
CHEMBL5175892 IC50 = 16.0 nM 7.80
CHEMBL5206613 IC50 = 20.0 nM 7.70
CHEMBL457614 IC50 = 20.0 nM 7.70
CHEMBL4856292 IC50 = 260.0 nM 6.58