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Assay Detail

CHEMBL4308455

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

Binding
Inhibition of human inactive TRKA assessed as decrease in substrate phosphorylation incubated for 2 hrs using CSKtide as substrate in presence of ATP measured every 5 minutes for 5 hrs by caliper method
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

Lead identification and characterization of hTrkA type 2 inhibitors.
Subramanian G, Zhu Y, Bowen SJ, Roush N, White JA, Huczek D, Zachary T, Javens C, Williams T, Janssen A, Gonzales A.
Bioorg Med Chem Lett (2019) 29 : 126680 -126680
PubMed 31610943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.06 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457614 1 8.43
CHEMBL4458913 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457614 Ki = 3.7 nM 8.43
CHEMBL4458913 Ki = 21.0 nM 7.68