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Assay Detail

CHEMBL3871570

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

Binding
Inhibition of wild type TTR (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs relative to control
6
Total Activities
6
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

Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
Kim B, Park H, Lee SK, Park SJ, Koo TS, Kang NS, Hong KB, Choi S.
Eur J Med Chem (2016) 123 : 777 -787
PubMed 27541261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.72 5.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3917629 1 5.83
CHEMBL2103837 TAFAMIDIS 4.0 1 5.81
CHEMBL3898378 1 5.72
CHEMBL3976323 1 5.69
CHEMBL3899454 1 5.66
CHEMBL3987064 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3917629 IC50 = 1490.0 nM 5.83
CHEMBL2103837 TAFAMIDIS IC50 = 1550.0 nM 5.81
CHEMBL3898378 IC50 = 1900.0 nM 5.72
CHEMBL3976323 IC50 = 2060.0 nM 5.69
CHEMBL3899454 IC50 = 2180.0 nM 5.66
CHEMBL3987064 IC50 = 2590.0 nM 5.59