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Assay Detail

CHEMBL2327238

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

Binding
Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Hypoxia-inducible factor 1-alpha (CHEMBL4261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors.
Minegishi H, Fukashiro S, Ban HS, Nakamura H.
ACS Med Chem Lett (2013) 4 : 297 -301
PubMed 24900662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.18 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2323956 1 7.85
CHEMBL2323957 1 7.47
CHEMBL253429 1 6.67
CHEMBL2323955 1 6.57
CHEMBL2323952 1 5.85
CHEMBL333985 1 5.82
CHEMBL2323954 1 5.50
CHEMBL2323953 1 5.21
CHEMBL427092 1 4.68
CHEMBL2323951 1 -
CHEMBL432219 1 -
CHEMBL2323950 1 -
CHEMBL371949 1 -
CHEMBL200726 1 -
CHEMBL371910 1 -
CHEMBL175596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2323956 IC50 = 14.0 nM 7.85
CHEMBL2323957 IC50 = 34.0 nM 7.47
CHEMBL253429 IC50 = 214.0 nM 6.67
CHEMBL2323955 IC50 = 270.0 nM 6.57
CHEMBL2323952 IC50 = 1400.0 nM 5.85
CHEMBL333985 IC50 = 1500.0 nM 5.82
CHEMBL2323954 IC50 = 3200.0 nM 5.50
CHEMBL2323953 IC50 = 6100.0 nM 5.21
CHEMBL427092 IC50 = 21000.0 nM 4.68
CHEMBL2323951 IC50 > 30000.0 nM -
CHEMBL432219 IC50 > 30000.0 nM -
CHEMBL2323950 IC50 > 30000.0 nM -
CHEMBL371949 IC50 > 30000.0 nM -
CHEMBL200726 IC50 > 30000.0 nM -
CHEMBL371910 IC50 > 30000.0 nM -
CHEMBL175596 IC50 > 30000.0 nM -