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Assay Detail

CHEMBL900187

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

Functional
Inhibition of transthyretin fibril formation at pH 4.4
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Transthyretin (CHEMBL3194)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of mechanism-based inhibitors of transthyretin amyloidosis: studies with biphenyl ethers and new structural templates.
Gupta S, Chhibber M, Sinha S, Surolia A.
J Med Chem (2007) 50 : 5589 -5599
PubMed 17948976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.33 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438498 1 6.32
CHEMBL240804 1 6.28
CHEMBL240805 1 6.07
CHEMBL394034 1 5.97
CHEMBL241453 1 5.88
CHEMBL240806 1 5.87
CHEMBL241025 1 5.71
CHEMBL240808 1 5.59
CHEMBL240165 1 5.51
CHEMBL241454 1 5.50
CHEMBL240807 1 5.50
CHEMBL559 DEXTROTHYROXINE 4.0 1 5.14
CHEMBL241575 1 4.70
CHEMBL241573 1 4.70
CHEMBL392872 1 4.39
CHEMBL238590 1 4.35
CHEMBL849 TRICLOSAN 4.0 1 4.27
CHEMBL392873 1 4.26
CHEMBL239010 1 -
CHEMBL241576 1 -
CHEMBL241574 1 -
CHEMBL241362 1 -
CHEMBL238802 1 -
CHEMBL238801 1 -
CHEMBL240949 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438498 IC50 = 475.0 nM 6.32
CHEMBL240804 IC50 = 520.0 nM 6.28
CHEMBL240805 IC50 = 850.0 nM 6.07
CHEMBL394034 IC50 = 1060.0 nM 5.97
CHEMBL241453 IC50 = 1310.0 nM 5.88
CHEMBL240806 IC50 = 1360.0 nM 5.87
CHEMBL241025 IC50 = 1940.0 nM 5.71
CHEMBL240808 IC50 = 2590.0 nM 5.59
CHEMBL240165 IC50 = 3100.0 nM 5.51
CHEMBL241454 IC50 = 3180.0 nM 5.50
CHEMBL240807 IC50 = 3160.0 nM 5.50
CHEMBL559 DEXTROTHYROXINE IC50 = 7170.0 nM 5.14
CHEMBL241575 IC50 = 20000.0 nM 4.70
CHEMBL241573 IC50 = 20000.0 nM 4.70
CHEMBL392872 IC50 = 41000.0 nM 4.39
CHEMBL238590 IC50 = 45000.0 nM 4.35
CHEMBL849 TRICLOSAN IC50 = 53500.0 nM 4.27
CHEMBL392873 IC50 = 55000.0 nM 4.26
CHEMBL239010 IC50 - -
CHEMBL241576 IC50 - -
CHEMBL241574 IC50 - -
CHEMBL241362 IC50 - -
CHEMBL238802 IC50 - -
CHEMBL238801 IC50 - -
CHEMBL240949 IC50 - -