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Assay Detail

CHEMBL4833461

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

Binding
Stabilization of TTR V30M mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance method
10
Total Activities
5
Compounds Tested
2
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
IC50 5 5.52 5.62
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290106 BITHIONOL 4.0 2 5.62
CHEMBL2103837 TAFAMIDIS 4.0 2 5.58
CHEMBL1324 TOLCAPONE 4.0 2 5.50
CHEMBL898 DIFLUNISAL 4.0 2 5.46
CHEMBL1086440 TRICLABENDAZOLE 4.0 2 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290106 BITHIONOL IC50 = 2400.0 nM 5.62
CHEMBL2103837 TAFAMIDIS IC50 = 2600.0 nM 5.58
CHEMBL1324 TOLCAPONE IC50 = 3200.0 nM 5.50
CHEMBL898 DIFLUNISAL IC50 = 3500.0 nM 5.46
CHEMBL1086440 TRICLABENDAZOLE IC50 = 3500.0 nM 5.46
CHEMBL2103837 TAFAMIDIS Activity - -
CHEMBL898 DIFLUNISAL Activity - -
CHEMBL1324 TOLCAPONE Activity - -
CHEMBL290106 BITHIONOL Activity - -
CHEMBL1086440 TRICLABENDAZOLE Activity - -