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Assay Detail

CHEMBL4359463

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

Binding
Inhibition of recombinant human His-tagged TRKA cytoplasmic domain (441 to 796 residues) expressed in baculovirus expression system using peptide substrate preincubated for 60 mins followed by substrate addition by microfluidic assay
1
Total Activities
1
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

Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.
Moccia M, Frett B, Zhang L, Lakkaniga NR, Briggs DC, Chauhan R, Brescia A, Federico G, Yan W, Santoro M, McDonald NQ, Li HY, Carlomagno F.
J Med Chem (2020) 63 : 4506 -4516
PubMed 32298114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4473213 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4473213 IC50 = 32.0 nM 7.50