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Assay Detail

CHEMBL4330196

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

Binding
Inhibition of TRKA G667C mutant (unknown origin) using poly-EAY peptide as substrate in presence of gamma-33ATP by LanthaScreen assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.
Yan W, Lakkaniga NR, Carlomagno F, Santoro M, McDonald NQ, Lv F, Gunaganti N, Frett B, Li HY.
J Med Chem (2019) 62 : 1731 -1760
PubMed 30188734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.18 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297627 SELITRECTINIB 2.0 1 9.01
CHEMBL3889654 LAROTRECTINIB 4.0 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297627 SELITRECTINIB IC50 = 0.98 nM 9.01
CHEMBL3889654 LAROTRECTINIB IC50 = 45.0 nM 7.35