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Assay Detail

CHEMBL4765712

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

Binding
Inhibition of GAL4 fused TrkB (unknown origin) expressed in MG87 cells transfected with pFA2-Elk plasmid and pFR-luciferase plasmid measured for 18 hrs by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MG87
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

BDNF/NT-3 growth factors receptor (CHEMBL4898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indole-like Trk receptor antagonists.
Tammiku-Taul J,Park R,Jaanson K,Luberg K,Dobchev DA,Kananovich D,Noole A,Mandel M,Kaasik A,Lopp M,Timmusk T,Karelson M
Eur J Med Chem (2016) 121 : 541 -552
PubMed 27318978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.07 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104519 1 7.39
CHEMBL104333 1 6.96
CHEMBL322153 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104519 IC50 = 41.07 nM 7.39
CHEMBL104333 IC50 = 110.95 nM 6.96
CHEMBL322153 IC50 = 141.83 nM 6.85