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Assay Detail

CHEMBL4309234

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

Binding
Antagonist activity at unphosphorylated rat TrkA expressed in baculovirus expression system preincubated for 20 mins followed by TK-substrate-Biotin addition and measured after 35 mins by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

High affinity nerve growth factor receptor (CHEMBL4220)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.
Bagal SK, Omoto K, Blakemore DC, Bungay PJ, Bilsland JG, Clarke PJ, Corbett MS, Cronin CN, Cui JJ, Dias R, Flanagan NJ, Greasley SE, Grimley R, Johnson E, Fengas D, Kitching L, Kraus ML, McAlpine I, Nagata A, Waldron GJ, Warmus JS.
J Med Chem (2018) 62 : 247 -265
PubMed 29672039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891994 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891994 IC50 = 6.0 nM 8.22