Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4765711

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

Binding
Inhibition of GAL4 fused TrkA (unknown origin) expressed in PC12 cells transfected with pFA2-Elk plasmid and pFR-luciferase plasmid measured for 18 hrs by luciferase reporter gene assay
24
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

High affinity nerve growth factor receptor (CHEMBL2815)
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 24 7.07 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457614 2 9.59
CHEMBL104519 2 8.00
CHEMBL104333 2 7.88
CHEMBL104279 2 7.43
CHEMBL322153 2 7.34
CHEMBL4798255 2 7.03
CHEMBL106226 2 6.99
CHEMBL321955 2 6.47
CHEMBL4788922 2 6.44
CHEMBL4074055 2 6.05
CHEMBL471375 2 6.00
CHEMBL476643 2 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457614 IC50 = 0.26 nM 9.59
CHEMBL457614 IC50 = 0.26 nM 9.59
CHEMBL104519 IC50 = 9.977 nM 8.00
CHEMBL104519 IC50 = 10.0 nM 8.00
CHEMBL104333 IC50 = 13.1 nM 7.88
CHEMBL104333 IC50 = 13.06 nM 7.88
CHEMBL104279 IC50 = 36.7 nM 7.43
CHEMBL104279 IC50 = 36.73 nM 7.43
CHEMBL322153 IC50 = 46.03 nM 7.34
CHEMBL322153 IC50 = 46.0 nM 7.34
CHEMBL4798255 IC50 = 92.8 nM 7.03
CHEMBL4798255 IC50 = 92.9 nM 7.03
CHEMBL106226 IC50 = 103.0 nM 6.99
CHEMBL106226 IC50 = 102.57 nM 6.99
CHEMBL321955 IC50 = 342.0 nM 6.47
CHEMBL321955 IC50 = 341.98 nM 6.47
CHEMBL4788922 IC50 = 366.0 nM 6.44
CHEMBL4788922 IC50 = 365.59 nM 6.44
CHEMBL4074055 IC50 = 887.16 nM 6.05
CHEMBL4074055 IC50 = 887.0 nM 6.05
CHEMBL471375 IC50 = 998.0 nM 6.00
CHEMBL471375 IC50 = 997.7 nM 6.00
CHEMBL476643 IC50 = 2760.0 nM 5.56
CHEMBL476643 IC50 = 2760.58 nM 5.56