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Assay Detail

CHEMBL1785939

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

Binding
Inhibition of HIF-1 in human deferoxamine treated HCT-116 cells expressing HRE-bla gene pretreated for 30 mins before deferoxamine challenge measured after 24 hrs by fluorometric analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HCT-116
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Toluidinesulfonamide hypoxia-induced factor 1 inhibitors: alleviating drug-drug interactions through use of PubChem data and comparative molecular field analysis guided synthesis.
Wendt B, Mulbaier M, Wawro S, Schultes C, Alonso J, Janssen B, Lewis J.
J Med Chem (2011) 54 : 3982 -3986
PubMed 21574568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.26 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1784702 1 7.40
CHEMBL1386228 1 7.20
CHEMBL1784701 1 7.00
CHEMBL1784700 1 6.20
CHEMBL1784699 1 5.80
CHEMBL1784698 1 5.50
CHEMBL1319809 1 4.70
CHEMBL1450745 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1784702 IC50 = 39.81 nM 7.40
CHEMBL1386228 IC50 = 63.1 nM 7.20
CHEMBL1784701 IC50 = 100.0 nM 7.00
CHEMBL1784700 IC50 = 630.96 nM 6.20
CHEMBL1784699 IC50 = 1584.89 nM 5.80
CHEMBL1784698 IC50 = 3162.28 nM 5.50
CHEMBL1319809 IC50 = 19952.62 nM 4.70
CHEMBL1450745 IC50 > 10000.0 nM -