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Assay Detail

CHEMBL1048170

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

Binding
Inhibition of TTR mediated fibrillogenesis assessed as acid-induced protein aggregation turbidity after 1.5 hrs by turbidimetric assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transthyretin (CHEMBL3194)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isatin derivatives, a novel class of transthyretin fibrillogenesis inhibitors.
González A, Quirante J, Nieto J, Almeida MR, Saraiva MJ, Planas A, Arsequell G, Valencia G.
Bioorg Med Chem Lett (2009) 19 : 5270 -5273
PubMed 19651509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.20 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570013 1 5.55
CHEMBL81721 TRIIODOPHENOL 1 5.50
CHEMBL60569 1 5.20
CHEMBL570239 1 5.20
CHEMBL570930 1 5.20
CHEMBL576310 1 5.11
CHEMBL378695 1 5.09
CHEMBL1624 LEVOTHYROXINE 4.0 1 4.98
CHEMBL571374 1 4.96
CHEMBL326294 ISATIN 1 -
CHEMBL227491 1 -
CHEMBL576111 1 -
CHEMBL570287 1 -
CHEMBL571597 1 -
CHEMBL571813 1 -
CHEMBL570847 1 -
CHEMBL577756 1 -
CHEMBL576687 1 -
CHEMBL570031 1 -
CHEMBL572224 1 -
CHEMBL572223 1 -
CHEMBL571589 1 -
CHEMBL571380 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570013 IC50 = 2800.0 nM 5.55
CHEMBL81721 TRIIODOPHENOL IC50 = 3200.0 nM 5.50
CHEMBL60569 IC50 = 6300.0 nM 5.20
CHEMBL570239 IC50 = 6300.0 nM 5.20
CHEMBL570930 IC50 = 6300.0 nM 5.20
CHEMBL576310 IC50 = 7700.0 nM 5.11
CHEMBL378695 IC50 = 8100.0 nM 5.09
CHEMBL1624 LEVOTHYROXINE IC50 = 10500.0 nM 4.98
CHEMBL571374 IC50 = 11000.0 nM 4.96
CHEMBL326294 ISATIN IC50 > 50000.0 nM -
CHEMBL227491 IC50 > 50000.0 nM -
CHEMBL576111 IC50 > 50000.0 nM -
CHEMBL570287 IC50 > 50000.0 nM -
CHEMBL571597 IC50 > 50000.0 nM -
CHEMBL571813 IC50 > 50000.0 nM -
CHEMBL570847 IC50 > 50000.0 nM -
CHEMBL577756 IC50 > 50000.0 nM -
CHEMBL576687 IC50 > 50000.0 nM -
CHEMBL570031 IC50 > 50000.0 nM -
CHEMBL572224 IC50 > 50000.0 nM -
CHEMBL572223 IC50 > 50000.0 nM -
CHEMBL571589 IC50 > 50000.0 nM -
CHEMBL571380 IC50 > 50000.0 nM -