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Assay Detail

CHEMBL5239595

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

Binding
Binding affinity to TTR V30M mutant (unknown origin) expressed in Escherichia coli by ITC assay
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

Chlorinated Naringenin Analogues as Potential Inhibitors of Transthyretin Amyloidogenesis.
Mizuguchi M, Nakagawa Y, Inui K, Katayama W, Sawai Y, Shimane A, Kitakami R, Okada T, Nabeshima Y, Yokoyama T, Kanamitsu K, Nakagawa S, Toyooka N.
J Med Chem (2022) 65 : 16218 -16233
PubMed 36472374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 7.28 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5276223 1 8.22
CHEMBL5268339 1 7.89
CHEMBL5283388 1 7.80
CHEMBL5280970 1 7.58
CHEMBL5290760 1 6.39
CHEMBL9352 NARINGENIN 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5276223 Kd = 6.0 nM 8.22
CHEMBL5268339 Kd = 13.0 nM 7.89
CHEMBL5283388 Kd = 16.0 nM 7.80
CHEMBL5280970 Kd = 26.0 nM 7.58
CHEMBL5290760 Kd = 403.0 nM 6.39
CHEMBL9352 NARINGENIN Kd = 1630.0 nM 5.79