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Assay Detail

CHEMBL5375276

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

Binding
Inhibition of recombinant N-terminal hexa-histidine tagged TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as acid mediated amyloid-like fibril formation by measuring turbidity incubated for 1 week at 310K in presence of sodium acetate by absorbance based assay
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

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
Ki 12 5.28 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL898 DIFLUNISAL 4.0 1 5.68
CHEMBL597744 TRIACETYLRESVERATROL 1 5.66
CHEMBL165 RESVERATROL 3.0 1 5.57
CHEMBL2103837 TAFAMIDIS 4.0 1 5.51
CHEMBL110370 1 5.50
CHEMBL498917 1 5.47
CHEMBL83527 PTEROSTILBENE 2.0 1 5.46
CHEMBL43065 OXYRESVERATROL 1 5.35
CHEMBL69863 PICEATANNOL 1 5.27
CHEMBL44509 (E)-3,4,3',5'-TETRAMETHOXYSTILBENE 1 4.31
CHEMBL5426941 1 4.27
CHEMBL296411 TRISMETHOXYRESVERATROL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL898 DIFLUNISAL Ki = 2100.0 nM 5.68
CHEMBL597744 TRIACETYLRESVERATROL Ki = 2200.0 nM 5.66
CHEMBL165 RESVERATROL Ki = 2700.0 nM 5.57
CHEMBL2103837 TAFAMIDIS Ki = 3100.0 nM 5.51
CHEMBL110370 Ki = 3200.0 nM 5.50
CHEMBL498917 Ki = 3400.0 nM 5.47
CHEMBL83527 PTEROSTILBENE Ki = 3500.0 nM 5.46
CHEMBL43065 OXYRESVERATROL Ki = 4500.0 nM 5.35
CHEMBL69863 PICEATANNOL Ki = 5400.0 nM 5.27
CHEMBL44509 (E)-3,4,3',5'-TETRAMETHOXYSTILBENE Ki = 49000.0 nM 4.31
CHEMBL5426941 Ki = 54000.0 nM 4.27
CHEMBL296411 TRISMETHOXYRESVERATROL Ki - -