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Assay Detail

CHEMBL5732024

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

Binding
TrkC Activity: Human TrkC, catalytic domain [456-825(end) amino acids of accession number NP_002521.2] was expressed as N-terminal GST-fusion protein (69 kDa) using baculovirus expression system. GST-TRKC was purified by using glutathione sepharose chromatography and stored in 50 mM Tris-HCl, 150 mM NaCl, 0.05% Brij35, 1 mM DTT, 10% glycerol, pH7.5 at −80 C. The kinase activity was measured by off-chip mobility shift assay. The enzyme was incubated with fluorecence-labeled substrate, Srctide, in the presence of 100 uM of ATP (Mg/or Mn)/ATP). The phosphorylated and unphosphorylated substrates were separated and detected by LabChip™3000.
3
Total Activities
1
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

NT-3 growth factor receptor (CHEMBL5608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tropomyosin-related kinase (TRK) inhibitors
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.30 9.30
kon 1 - -
k_off 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3673452 GZ-389988 2.0 3 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3673452 GZ-389988 IC50 = 0.503 nM 9.30
CHEMBL3673452 GZ-389988 kon = - -
CHEMBL3673452 GZ-389988 k_off = - s-1 -