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Assay Detail

CHEMBL5327390

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

Binding
Binding affinity to thyroxin binding site of TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as quenching of intrinsic tryptophan fluorescence by measuring apparent dissociation constant incubated for 60 mins by fluorescence based analysis
4
Total Activities
4
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

Benziodarone and 6-hydroxybenziodarone are potent and selective inhibitors of transthyretin amyloidogenesis.
Mizuguchi M, Yokoyama T, Okada T, Nakagawa Y, Fujii K, Nabeshima Y, Toyooka N.
Bioorg Med Chem (2023) 90 : 117370 -117370
PubMed 37311373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.41 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388590 BENZBROMARONE 4.0 1 6.70
CHEMBL232201 BENZIODARONE 4.0 1 6.39
CHEMBL5422596 1 6.39
CHEMBL1767079 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388590 BENZBROMARONE Kd = 200.0 nM 6.70
CHEMBL232201 BENZIODARONE Kd = 410.0 nM 6.39
CHEMBL5422596 Kd = 410.0 nM 6.39
CHEMBL1767079 Kd = 700.0 nM 6.16