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Assay Detail

CHEMBL4833467

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

Binding
Binding affinity to TTR V30M mutant (unknown origin) by isothermal titration calorimetry
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

Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
Yokoyama T, Kashihara M, Mizuguchi M.
J Med Chem (2021) 64 : 14344 -14357
PubMed 34547896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.71 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290106 BITHIONOL 4.0 1 7.21
CHEMBL1324 TOLCAPONE 4.0 1 7.02
CHEMBL2103837 TAFAMIDIS 4.0 1 6.70
CHEMBL898 DIFLUNISAL 4.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290106 BITHIONOL Kd = 62.0 nM 7.21
CHEMBL1324 TOLCAPONE Kd = 95.0 nM 7.02
CHEMBL2103837 TAFAMIDIS Kd = 200.0 nM 6.70
CHEMBL898 DIFLUNISAL Kd = 1300.0 nM 5.89