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Assay Detail

CHEMBL4833458

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

Binding
Binding affinity to TTR V30M mutant (unknown origin) expressed in Escherichia coli incubated for 60 mins by tryptophan intrinsic fluorescence 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
Kd 5 5.47 6.01
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1324 TOLCAPONE 4.0 2 6.01
CHEMBL290106 BITHIONOL 4.0 2 5.96
CHEMBL5416410 DASATINIB 4.0 2 5.51
CHEMBL4847991 2 5.19
CHEMBL1096 AMLEXANOX 4.0 2 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1324 TOLCAPONE Kd = 980.0 nM 6.01
CHEMBL290106 BITHIONOL Kd = 1100.0 nM 5.96
CHEMBL5416410 DASATINIB Kd = 3100.0 nM 5.51
CHEMBL4847991 Kd = 6500.0 nM 5.19
CHEMBL1096 AMLEXANOX Kd = 20000.0 nM 4.70
CHEMBL1324 TOLCAPONE Activity - -
CHEMBL4847991 Activity - -
CHEMBL1096 AMLEXANOX Activity - -
CHEMBL5416410 DASATINIB Activity - -
CHEMBL290106 BITHIONOL Activity - -