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Assay Detail

CHEMBL5223531

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Binding
Inhibition of acid-induced fibrillogenesis of human Transthyretin Y78F mutant expressed in Escherichia coli BL21 (DE3) cells assessed as inhibition of fibril formation incubated for 30 mins by kinetic turbidimetric assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimization of kinetic stabilizers of tetrameric transthyretin: A prospective ligand efficiency-guided approach.
Cotrina EY, Blasi D, Vilà M, Planas A, Abad-Zapatero C, Centeno NB, Quintana J, Arsequell G.
Bioorg Med Chem (2020) 28 : 115794 -115794
PubMed 33091848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.22 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5284574 1 5.44
CHEMBL5287212 1 5.43
CHEMBL5271162 1 5.41
CHEMBL1232738 1 5.38
CHEMBL5278455 1 5.37
CHEMBL5291276 1 5.34
CHEMBL5276015 1 5.29
CHEMBL5276384 1 5.28
CHEMBL5278846 1 5.28
CHEMBL5283682 1 5.22
CHEMBL5272582 1 5.22
CHEMBL5278451 1 5.21
CHEMBL5270535 1 5.14
CHEMBL5273376 1 5.14
CHEMBL5275465 1 4.66
CHEMBL5266565 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5284574 IC50 = 3600.0 nM 5.44
CHEMBL5287212 IC50 = 3700.0 nM 5.43
CHEMBL5271162 IC50 = 3900.0 nM 5.41
CHEMBL1232738 IC50 = 4200.0 nM 5.38
CHEMBL5278455 IC50 = 4300.0 nM 5.37
CHEMBL5291276 IC50 = 4600.0 nM 5.34
CHEMBL5276015 IC50 = 5100.0 nM 5.29
CHEMBL5276384 IC50 = 5300.0 nM 5.28
CHEMBL5278846 IC50 = 5200.0 nM 5.28
CHEMBL5283682 IC50 = 6000.0 nM 5.22
CHEMBL5272582 IC50 = 6000.0 nM 5.22
CHEMBL5278451 IC50 = 6100.0 nM 5.21
CHEMBL5270535 IC50 = 7200.0 nM 5.14
CHEMBL5273376 IC50 = 7200.0 nM 5.14
CHEMBL5275465 IC50 = 21700.0 nM 4.66
CHEMBL5266565 IC50 = 23100.0 nM 4.64