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Assay Detail

CHEMBL3862353

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

Binding
Binding affinity to recombinant human wild type TTR expressed in Escherichia coli BL21 (DE3) assessed as dissociation constants for second binding site of TTR by isothermal titration calorimetric method
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

A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
Simões CJV, Almeida ZL, Costa D, Jesus CSH, Cardoso AL, Almeida MR, Saraiva MJ, Pinho E Melo TMVD, Brito RMM.
Eur J Med Chem (2016) 121 : 823 -840
PubMed 27020050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.52 6.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103837 TAFAMIDIS 4.0 1 6.56
CHEMBL3890392 1 6.56
CHEMBL3959466 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103837 TAFAMIDIS Kd = 274.0 nM 6.56
CHEMBL3890392 Kd = 278.0 nM 6.56
CHEMBL3959466 Kd = 357.0 nM 6.45