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Assay Detail

CHEMBL4019935

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

Binding
Competitive binding affinity to human wild type TTR expressed in Escherichia coli BL-21 assessed as equilibrium dissociation constant of second site in presence of ANS by spectrofluorometer
12
Total Activities
12
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

Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
Smith TP, Windsor IW, Forest KT, Raines RT.
J Med Chem (2017) 60 : 7820 -7834
PubMed 28920684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 6.21 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103837 TAFAMIDIS 4.0 1 6.43
CHEMBL4072121 1 6.36
CHEMBL4090439 1 6.35
CHEMBL4078202 1 6.33
CHEMBL4069407 1 6.33
CHEMBL165 RESVERATROL 3.0 1 6.33
CHEMBL4063503 1 6.33
CHEMBL4099088 1 6.14
CHEMBL4065175 1 6.10
CHEMBL4102478 1 6.09
CHEMBL4082603 1 6.00
CHEMBL4060726 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103837 TAFAMIDIS Kd = 370.0 nM 6.43
CHEMBL4072121 Kd = 440.0 nM 6.36
CHEMBL4090439 Kd = 450.0 nM 6.35
CHEMBL4078202 Kd = 470.0 nM 6.33
CHEMBL4069407 Kd = 470.0 nM 6.33
CHEMBL165 RESVERATROL Kd = 470.0 nM 6.33
CHEMBL4063503 Kd = 470.0 nM 6.33
CHEMBL4099088 Kd = 730.0 nM 6.14
CHEMBL4065175 Kd = 790.0 nM 6.10
CHEMBL4102478 Kd = 820.0 nM 6.09
CHEMBL4082603 Kd = 990.0 nM 6.00
CHEMBL4060726 Kd = 1800.0 nM 5.75