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Assay Detail

CHEMBL5549067

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

Binding
Binding affinity to TTR V30M mutant (unknown origin) assessed as dissociation constant by ITC analysis
7
Total Activities
7
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

Development of Benziodarone Analogues with Enhanced Potency for Selective Binding to Transthyretin in Human Plasma.
Mizuguchi M, Nakagawa Y, Yokoyama T, Okada T, Fujii K, Takahashi K, Luan NNT, Nabeshima Y, Kanamitsu K, Nakagawa S, Yamakawa S, Ueda M, Ando Y, Toyooka N.
J Med Chem (2024) 67 : 6987 -7005
PubMed 38670538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 7.16 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5575152 1 7.40
CHEMBL5570538 1 7.38
CHEMBL5573622 1 7.28
CHEMBL5566935 1 7.18
CHEMBL232201 BENZIODARONE 4.0 1 7.11
CHEMBL5570396 1 6.92
CHEMBL2103837 TAFAMIDIS 4.0 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5575152 Kd = 40.0 nM 7.40
CHEMBL5570538 Kd = 42.0 nM 7.38
CHEMBL5573622 Kd = 53.0 nM 7.28
CHEMBL5566935 Kd = 66.0 nM 7.18
CHEMBL232201 BENZIODARONE Kd = 78.0 nM 7.11
CHEMBL5570396 Kd = 120.0 nM 6.92
CHEMBL2103837 TAFAMIDIS Kd = 138.0 nM 6.86