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Assay Detail

CHEMBL808365

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

Binding
Ability to inhibit human trk A tyrosine kinase expressed in baculovirus using ELISA based enzyme assay was determined
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives.
Kaneko M, Saito Y, Saito H, Matsumoto T, Matsuda Y, Vaught JL, Dionne CA, Angeles TS, Glicksman MA, Neff NT, Rotella DP, Kauer JC, Mallamo JP, Hudkins RL, Murakata C.
J Med Chem (1997) 40 : 1863 -1869
PubMed 9191963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.29 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281948 K-252A 1 8.62
CHEMBL53885 1 6.68
CHEMBL291985 1 6.57
CHEMBL444039 1 -
CHEMBL55567 1 -
CHEMBL301144 1 -
CHEMBL433281 1 -
CHEMBL299496 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281948 K-252A IC50 = 2.4 nM 8.62
CHEMBL53885 IC50 = 210.0 nM 6.68
CHEMBL291985 IC50 = 270.0 nM 6.57
CHEMBL444039 IC50 > 1000.0 nM -
CHEMBL55567 IC50 > 1000.0 nM -
CHEMBL301144 IC50 > 1000.0 nM -
CHEMBL433281 IC50 > 1000.0 nM -
CHEMBL299496 IC50 > 1000.0 nM -