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Assay Detail

CHEMBL4309198

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

Binding
Binding affinity to C-terminal-His6/N-terminal BAP-tagged unphosphorylated TrkA (unknown origin) (441 to 796 residues) by SPR analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

High affinity nerve growth factor receptor (CHEMBL2815)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Kd 2 7.74 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891994 1 8.38
CHEMBL4460719 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891994 Kd = 4.2 nM 8.38
CHEMBL4460719 Kd = 80.0 nM 7.10