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Assay Detail

CHEMBL4404793

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

Binding
Stabilization of wild type human transthyretin expressed in Escherichia coli BL21(DE3) Star assessed as dissociation constant for TTR-amyloid beta (12 to 28) complex formation at 200 uM at 25 degC pre-incubated with transthyretin before amyloid beta (12 to 28) addition by ITC assay (Rvb = 3 +/- 0.2 microM)
3
Total Activities
3
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

Calorimetric Studies of Binary and Ternary Molecular Interactions between Transthyretin, Aβ Peptides, and Small-Molecule Chaperones toward an Alternative Strategy for Alzheimer's Disease Drug Discovery.
Cotrina EY, Gimeno A, Llop J, Jiménez-Barbero J, Quintana J, Valencia G, Cardoso I, Prohens R, Arsequell G.
J Med Chem (2020) 63 : 3205 -3214
PubMed 32124607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 5.74 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1232738 1 6.09
CHEMBL898 DIFLUNISAL 4.0 1 5.57
CHEMBL2103837 TAFAMIDIS 4.0 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1232738 Kd = 810.0 nM 6.09
CHEMBL898 DIFLUNISAL Kd = 2700.0 nM 5.57
CHEMBL2103837 TAFAMIDIS Kd = 2800.0 nM 5.55