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Assay Detail

CHEMBL5549064

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

Binding
Binding affinity to TTR in human plasma assessed as target occupancy incubated for 6 hrs in presence of E)-S-phenyl 3-(4-hydroxy-3,5-dimethyistyryl)benzothioate by fluorescence based competitive binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
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
EC50 7 5.35 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566935 1 5.60
CHEMBL5570538 1 5.57
CHEMBL5575152 1 5.52
CHEMBL5570396 1 5.46
CHEMBL5573622 1 5.41
CHEMBL232201 BENZIODARONE 4.0 1 5.05
CHEMBL2103837 TAFAMIDIS 4.0 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566935 EC50 = 2500.0 nM 5.60
CHEMBL5570538 EC50 = 2700.0 nM 5.57
CHEMBL5575152 EC50 = 3000.0 nM 5.52
CHEMBL5570396 EC50 = 3500.0 nM 5.46
CHEMBL5573622 EC50 = 3900.0 nM 5.41
CHEMBL232201 BENZIODARONE EC50 = 8900.0 nM 5.05
CHEMBL2103837 TAFAMIDIS EC50 = 15600.0 nM 4.81