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Assay Detail

CHEMBL5375277

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

Binding
Binding affinity to recombinant N-terminal hexa-histidine tagged TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as quenching of intrinsic tryptophan fluorescence by measuring apparent dissociation constant incubated for 60 mins by fluorescence based analysis
12
Total Activities
12
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

Resveratrol Derivatives Inhibit Transthyretin Fibrillization: Structural Insights into the Interactions between Resveratrol Derivatives and Transthyretin.
Yokoyama T, Kusaka K, Mizuguchi M, Nabeshima Y, Fujiwara S.
J Med Chem (2023) 66 : 15511 -15523
PubMed 37910439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 5.59 6.14
Kd(app) 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110370 1 6.14
CHEMBL498917 1 5.92
CHEMBL165 RESVERATROL 3.0 1 5.85
CHEMBL83527 PTEROSTILBENE 2.0 1 5.72
CHEMBL69863 PICEATANNOL 1 5.68
CHEMBL43065 OXYRESVERATROL 1 5.62
CHEMBL296411 TRISMETHOXYRESVERATROL 1 5.39
CHEMBL44509 (E)-3,4,3',5'-TETRAMETHOXYSTILBENE 1 5.16
CHEMBL5426941 1 4.85
CHEMBL2103837 TAFAMIDIS 4.0 1 -
CHEMBL898 DIFLUNISAL 4.0 1 -
CHEMBL597744 TRIACETYLRESVERATROL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110370 Kd = 730.0 nM 6.14
CHEMBL498917 Kd = 1200.0 nM 5.92
CHEMBL165 RESVERATROL Kd = 1400.0 nM 5.85
CHEMBL83527 PTEROSTILBENE Kd = 1900.0 nM 5.72
CHEMBL69863 PICEATANNOL Kd = 2100.0 nM 5.68
CHEMBL43065 OXYRESVERATROL Kd = 2400.0 nM 5.62
CHEMBL296411 TRISMETHOXYRESVERATROL Kd = 4100.0 nM 5.39
CHEMBL44509 (E)-3,4,3',5'-TETRAMETHOXYSTILBENE Kd = 6900.0 nM 5.16
CHEMBL5426941 Kd = 14000.0 nM 4.85
CHEMBL2103837 TAFAMIDIS Kd(app) - -
CHEMBL898 DIFLUNISAL Kd(app) - -
CHEMBL597744 TRIACETYLRESVERATROL Kd(app) - -