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Assay Detail

CHEMBL4765818

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

Binding
Inhibition of GST-fused TrkA (unknown origin) expressed in SF9 cells using H2N-RRRAAAEEIYGEINH2 peptide as substrate preincubated with ATP and Mg and measured by microtiter plate reader analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
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 10 7.99 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176544 1 8.70
CHEMBL175321 1 8.22
CHEMBL1794058 GW278681X 1 8.22
CHEMBL1794057 GW284408X 1 8.15
CHEMBL1794056 GW301789X 1 8.10
CHEMBL176857 GW442130X 1 8.10
CHEMBL1276446 1 8.05
CHEMBL172179 1 7.92
CHEMBL369490 1 7.21
CHEMBL269850 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176544 IC50 = 2.0 nM 8.70
CHEMBL175321 IC50 = 6.0 nM 8.22
CHEMBL1794058 GW278681X IC50 = 6.0 nM 8.22
CHEMBL1794057 GW284408X IC50 = 7.0 nM 8.15
CHEMBL1794056 GW301789X IC50 = 8.0 nM 8.10
CHEMBL176857 GW442130X IC50 = 8.0 nM 8.10
CHEMBL1276446 IC50 = 9.0 nM 8.05
CHEMBL172179 IC50 = 12.0 nM 7.92
CHEMBL369490 IC50 = 61.0 nM 7.21
CHEMBL269850 IC50 = 63.0 nM 7.20