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Assay Detail

CHEMBL5582001

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Functional
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay
6
Total Activities
6
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 novel indazole derivatives as second-generation TRK inhibitors.
Qin Q, Lu S, Guo Z, Li Z, Fu Q, Wang X, Wu T, Sun Y, Liu N, Zhang H, Zhao D, Cheng M.
Eur J Med Chem (2024) 276 : 116640 -116640
PubMed 39033612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.48 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5592878 1 8.33
CHEMBL4297627 SELITRECTINIB 2.0 1 7.92
CHEMBL5594862 1 7.89
CHEMBL5594048 1 7.26
CHEMBL5593896 1 6.88
CHEMBL5594742 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5592878 IC50 = 4.7 nM 8.33
CHEMBL4297627 SELITRECTINIB IC50 = 12.0 nM 7.92
CHEMBL5594862 IC50 = 13.0 nM 7.89
CHEMBL5594048 IC50 = 54.5 nM 7.26
CHEMBL5593896 IC50 = 131.8 nM 6.88
CHEMBL5594742 IC50 = 253.9 nM 6.59