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Assay Detail

CHEMBL4200690

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

Binding
Binding affinity to transthyretin (unknown origin) by ITC method
8
Total Activities
8
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

Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis.
Miller M, Pal A, Albusairi W, Joo H, Pappas B, Haque Tuhin MT, Liang D, Jampala R, Liu F, Khan J, Faaij M, Park M, Chan W, Graef I, Zamboni R, Kumar N, Fox J, Sinha U, Alhamadsheh M.
J Med Chem (2018) 61 : 7862 -7876
PubMed 30133284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 7.11 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103837 TAFAMIDIS 4.0 1 8.36
CHEMBL3940890 ACORAMIDIS 4.0 1 8.32
CHEMBL1324 TOLCAPONE 4.0 1 7.69
CHEMBL4206443 1 7.05
CHEMBL4210824 1 6.60
CHEMBL4218173 1 6.59
CHEMBL898 DIFLUNISAL 4.0 1 6.39
CHEMBL4205939 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103837 TAFAMIDIS Kd = 4.4 nM 8.36
CHEMBL3940890 ACORAMIDIS Kd = 4.8 nM 8.32
CHEMBL1324 TOLCAPONE Kd = 20.6 nM 7.69
CHEMBL4206443 Kd = 90.0 nM 7.05
CHEMBL4210824 Kd = 251.0 nM 6.60
CHEMBL4218173 Kd = 258.0 nM 6.59
CHEMBL898 DIFLUNISAL Kd = 407.0 nM 6.39
CHEMBL4205939 Kd = 1253.0 nM 5.90