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Assay Detail

CHEMBL5033187

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

Binding
Disruption of retional-induced bacterially expressed MBP-tagged RBP4-TTR (unknown origin) protein-protein interaction measured by d2 dye based HTFR assay
15
Total Activities
15
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

Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities.
Cioffi CL, Raja A, Muthuraman P, Jayaraman A, Jayakumar S, Varadi A, Racz B, Petrukhin K.
J Med Chem (2021) 64 : 9010 -9041
PubMed 34138572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.67 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3940890 ACORAMIDIS 4.0 1 6.29
CHEMBL5082796 1 6.23
CHEMBL5080175 1 6.07
CHEMBL2103837 TAFAMIDIS 4.0 1 6.01
CHEMBL5091368 1 5.76
CHEMBL5089170 1 5.58
CHEMBL5080942 1 5.45
CHEMBL5093498 1 5.02
CHEMBL5085751 1 4.62
CHEMBL5078773 1 -
CHEMBL5090952 1 -
CHEMBL5091475 1 -
CHEMBL5081258 1 -
CHEMBL5089791 1 -
CHEMBL5082364 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3940890 ACORAMIDIS IC50 = 512.0 nM 6.29
CHEMBL5082796 IC50 = 583.0 nM 6.23
CHEMBL5080175 IC50 = 845.0 nM 6.07
CHEMBL2103837 TAFAMIDIS IC50 = 981.0 nM 6.01
CHEMBL5091368 IC50 = 1740.0 nM 5.76
CHEMBL5089170 IC50 = 2650.0 nM 5.58
CHEMBL5080942 IC50 = 3560.0 nM 5.45
CHEMBL5093498 IC50 = 9580.0 nM 5.02
CHEMBL5085751 IC50 = 24010.0 nM 4.62
CHEMBL5078773 IC50 - -
CHEMBL5090952 IC50 - -
CHEMBL5091475 IC50 - -
CHEMBL5081258 IC50 - -
CHEMBL5089791 IC50 - -
CHEMBL5082364 IC50 - -