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Assay Detail

CHEMBL3130350

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

Binding
Inhibition of transthyretin V30M mutant (unknown origin) expressed in Escherichia coli assessed as inhibition of sodium acetate-mediated aggregation preincubated for 30 mins followed by sodium acetate addition measured after 96 hrs by thioflavin T assay
6
Total Activities
6
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

Transthyretin (CHEMBL3194)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Crystal structures of human transthyretin complexed with glabridin.
Yokoyama T, Kosaka Y, Mizuguchi M.
J Med Chem (2014) 57 : 1090 -1096
PubMed 24422526 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.06 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL898 DIFLUNISAL 4.0 1 5.20
CHEMBL151 LUTEOLIN 2.0 1 5.19
CHEMBL480477 GLABRIDIN 1 5.19
CHEMBL44 GENISTEIN 2.0 1 5.11
CHEMBL3127843 1 4.89
CHEMBL8145 DAIDZEIN 2.0 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL898 DIFLUNISAL IC50 = 6300.0 nM 5.20
CHEMBL151 LUTEOLIN IC50 = 6400.0 nM 5.19
CHEMBL480477 GLABRIDIN IC50 = 6400.0 nM 5.19
CHEMBL44 GENISTEIN IC50 = 7800.0 nM 5.11
CHEMBL3127843 IC50 = 13000.0 nM 4.89
CHEMBL8145 DAIDZEIN IC50 = 16000.0 nM 4.80