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Assay Detail

CHEMBL3602659

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

Binding
Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Transthyretin (CHEMBL3194)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.
Iakovleva I, Brännström K, Nilsson L, Gharibyan AL, Begum A, Anan I, Walfridsson M, Sauer-Eriksson AE, Olofsson A.
J Med Chem (2015) 58 : 6507 -6515
PubMed 26214366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.64 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151 LUTEOLIN 2.0 1 5.16
CHEMBL28 APIGENIN 1 4.75
CHEMBL898 DIFLUNISAL 4.0 1 4.60
CHEMBL121626 TOLFENAMIC ACID 2.0 1 4.40
CHEMBL509 MECLOFENAMIC ACID 4.0 1 4.30
CHEMBL457 GEMFIBROZIL 4.0 1 -
CHEMBL93645 ACECLOFENAC 2.0 1 -
CHEMBL139 DICLOFENAC 4.0 1 -
CHEMBL63323 NIFLUMIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151 LUTEOLIN IC50 = 7000.0 nM 5.16
CHEMBL28 APIGENIN IC50 = 18000.0 nM 4.75
CHEMBL898 DIFLUNISAL IC50 = 25000.0 nM 4.60
CHEMBL121626 TOLFENAMIC ACID IC50 = 40000.0 nM 4.40
CHEMBL509 MECLOFENAMIC ACID IC50 = 50000.0 nM 4.30
CHEMBL457 GEMFIBROZIL IC50 = 180000.0 nM -
CHEMBL93645 ACECLOFENAC IC50 = 170000.0 nM -
CHEMBL139 DICLOFENAC IC50 = 140000.0 nM -
CHEMBL63323 NIFLUMIC ACID IC50 = 130000.0 nM -