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Assay Detail

CHEMBL5380377

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

Binding
Inhibition of His-tagged human recombinant wild type TRKA
3
Total Activities
3
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

Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.
Acharya B, Saha D, Armstrong D, Jabali B, Hanafi M, Herrera-Rueda A, Lakkaniga NR, Frett B.
RSC Med Chem (2024) 15 : 399 -415
PubMed 38389874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.18 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5400169 1 9.27
CHEMBL4297627 SELITRECTINIB 2.0 1 9.22
CHEMBL3889654 LAROTRECTINIB 4.0 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5400169 IC50 = 0.533 nM 9.27
CHEMBL4297627 SELITRECTINIB IC50 = 0.6 nM 9.22
CHEMBL3889654 LAROTRECTINIB IC50 = 0.9 nM 9.05