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Assay Detail

CHEMBL900184

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

Binding
Binding affinity to transthyretin at pH 4.4
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct 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
Kd 13 7.98 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438498 1 9.70
CHEMBL240806 1 9.52
CHEMBL240805 1 8.24
CHEMBL240804 1 7.86
CHEMBL241454 1 7.57
CHEMBL240808 1 7.57
CHEMBL240165 1 7.38
CHEMBL241453 1 7.06
CHEMBL394034 1 6.92
CHEMBL849 TRICLOSAN 4.0 1 -
CHEMBL559 DEXTROTHYROXINE 4.0 1 -
CHEMBL241025 1 -
CHEMBL240807 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438498 Kd = 0.2 nM 9.70
CHEMBL240806 Kd = 0.3 nM 9.52
CHEMBL240805 Kd = 5.7 nM 8.24
CHEMBL240804 Kd = 13.9 nM 7.86
CHEMBL241454 Kd = 27.0 nM 7.57
CHEMBL240808 Kd = 27.0 nM 7.57
CHEMBL240165 Kd = 42.0 nM 7.38
CHEMBL241453 Kd = 88.0 nM 7.06
CHEMBL394034 Kd = 120.0 nM 6.92
CHEMBL849 TRICLOSAN Kd = 144000.0 nM -
CHEMBL559 DEXTROTHYROXINE Kd - -
CHEMBL241025 Kd - -
CHEMBL240807 Kd - -