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Assay Detail

CHEMBL3377077

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

Binding
Inhibition of TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as inhibition of amyloid fibril formation by fluorescence assay
16
Total Activities
16
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

Inhibitory activities of propolis and its promising component, caffeic acid phenethyl ester, against amyloidogenesis of human transthyretin.
Yokoyama T, Kosaka Y, Mizuguchi M.
J Med Chem (2014) 57 : 8928 -8935
PubMed 25314129 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 4.79 5.25
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL898 DIFLUNISAL 4.0 1 5.25
CHEMBL1976696 DIHYDROGUAIARETIC ACID 1 5.20
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 5.14
CHEMBL442022 1 5.10
CHEMBL324842 ROSMARINIC ACID 1 5.07
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER 1 5.07
CHEMBL131680 1 4.96
CHEMBL133714 BENZYL CAFFEATE 1 4.80
CHEMBL471184 PRENYL CAFFEATE 1 4.68
CHEMBL17347 ETHYL CAFFEATE 1 4.64
CHEMBL133642 1 4.24
CHEMBL17001 METHYLCAFFEATE 1 4.17
CHEMBL145 CAFFEIC ACID 3.0 1 4.01
CHEMBL284616 CHLOROGENIC ACID 2.0 1 -
CHEMBL493921 PHENETHYL CINNAMATE 1 -
CHEMBL492149 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL898 DIFLUNISAL EC50 = 5600.0 nM 5.25
CHEMBL1976696 DIHYDROGUAIARETIC ACID EC50 = 6300.0 nM 5.20
CHEMBL52 NORDIHYDROGUAIARETIC ACID EC50 = 7300.0 nM 5.14
CHEMBL442022 EC50 = 7900.0 nM 5.10
CHEMBL324842 ROSMARINIC ACID EC50 = 8600.0 nM 5.07
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER EC50 = 8600.0 nM 5.07
CHEMBL131680 EC50 = 11000.0 nM 4.96
CHEMBL133714 BENZYL CAFFEATE EC50 = 16000.0 nM 4.80
CHEMBL471184 PRENYL CAFFEATE EC50 = 21000.0 nM 4.68
CHEMBL17347 ETHYL CAFFEATE EC50 = 23000.0 nM 4.64
CHEMBL133642 EC50 = 58000.0 nM 4.24
CHEMBL17001 METHYLCAFFEATE EC50 = 67000.0 nM 4.17
CHEMBL145 CAFFEIC ACID EC50 = 97000.0 nM 4.01
CHEMBL284616 CHLOROGENIC ACID Inhibition - % -
CHEMBL493921 PHENETHYL CINNAMATE Inhibition - % -
CHEMBL492149 EC50 - -