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Assay Detail

CHEMBL5164786

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

Binding
Inhibition of wild type CD74 fused TRKA (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of TRKA phosphorylation incubated for 6 hrs by Western blot analysis
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

High affinity nerve growth factor receptor (CHEMBL2815)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Wang Z, Wang J, Wang Y, Xiang S, Song X, Tu Z, Zhou Y, Zhang ZM, Zhang Z, Ding K, Lu X.
J Med Chem (2022) 65 : 6325 -6337
PubMed 35426680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.90 7.90
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5195469 2 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5195469 IC50 = 12.5 nM 7.90
CHEMBL5195469 Inhibition - % -