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Assay Detail

CHEMBL3869978

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

Binding
Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha (CHEMBL2221345)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Development of 1-aryl-3-furanyl/thienyl-imidazopyridine templates for inhibitors against hypoxia inducible factor (HIF)-1 transcriptional activity.
Fuse S, Ohuchi T, Asawa Y, Sato S, Nakamura H.
Bioorg Med Chem Lett (2016) 26 : 5887 -5890
PubMed 27847273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.79 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333985 1 5.92
CHEMBL3927498 1 5.43
CHEMBL3899458 1 5.19
CHEMBL3918550 1 5.13
CHEMBL3936460 1 5.04
CHEMBL3908512 1 5.03
CHEMBL3918157 1 4.77
CHEMBL3915177 1 4.60
CHEMBL3946046 1 4.41
CHEMBL3892315 1 4.25
CHEMBL3918408 1 4.21
CHEMBL3961295 1 4.16
CHEMBL3940432 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333985 IC50 = 1200.0 nM 5.92
CHEMBL3927498 IC50 = 3700.0 nM 5.43
CHEMBL3899458 IC50 = 6500.0 nM 5.19
CHEMBL3918550 IC50 = 7400.0 nM 5.13
CHEMBL3936460 IC50 = 9100.0 nM 5.04
CHEMBL3908512 IC50 = 9400.0 nM 5.03
CHEMBL3918157 IC50 = 17000.0 nM 4.77
CHEMBL3915177 IC50 = 25000.0 nM 4.60
CHEMBL3946046 IC50 = 39000.0 nM 4.41
CHEMBL3892315 IC50 = 56000.0 nM 4.25
CHEMBL3918408 IC50 = 61000.0 nM 4.21
CHEMBL3961295 IC50 = 70000.0 nM 4.16
CHEMBL3940432 IC50 = 75000.0 nM 4.12