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Assay Detail

CHEMBL5549065

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

Binding
Inhibition of acid-induced TTR V30M mutant (unknown origin) aggregation preincubated for 30 mins followed by acetate buffer at pH 4.7 addition and measured after 7 days by thioflavin T based fluorescence analysis
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

Development of Benziodarone Analogues with Enhanced Potency for Selective Binding to Transthyretin in Human Plasma.
Mizuguchi M, Nakagawa Y, Yokoyama T, Okada T, Fujii K, Takahashi K, Luan NNT, Nabeshima Y, Kanamitsu K, Nakagawa S, Yamakawa S, Ueda M, Ando Y, Toyooka N.
J Med Chem (2024) 67 : 6987 -7005
PubMed 38670538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.25 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566935 1 5.30
CHEMBL5570538 1 5.28
CHEMBL5573622 1 5.27
CHEMBL5575152 1 5.21
CHEMBL5570396 1 5.19
CHEMBL388590 BENZBROMARONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566935 IC50 = 5000.0 nM 5.30
CHEMBL5570538 IC50 = 5200.0 nM 5.28
CHEMBL5573622 IC50 = 5400.0 nM 5.27
CHEMBL5575152 IC50 = 6100.0 nM 5.21
CHEMBL5570396 IC50 = 6500.0 nM 5.19
CHEMBL388590 BENZBROMARONE IC50 ~ 5000.0 nM -