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Assay Detail

CHEMBL5250529

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

Functional
Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method
3
Total Activities
3
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

1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions.
Zhang Y, Chan S, He R, Liu Y, Song X, Tu ZC, Ren X, Zhou Y, Zhang Z, Wang Z, Zhou F, Ding K.
Eur J Med Chem (2022) 244 : 114862 -114862
PubMed 36308779 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.62 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5291008 1 7.27
CHEMBL4582651 PRALSETINIB 4.0 1 6.67
CHEMBL4559134 SELPERCATINIB 4.0 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5291008 IC50 = 54.2 nM 7.27
CHEMBL4582651 PRALSETINIB IC50 = 215.0 nM 6.67
CHEMBL4559134 SELPERCATINIB IC50 = 1242.0 nM 5.91