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Assay Detail

CHEMBL3625035

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

Binding
Inhibition of HIF1 in human HEK293T cells transfected with pGL3-5HRE-VEGF and pRL-SV40 after 24 hrs by dual luciferase reporter assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
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

Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1α Inhibition.
Kwon DY, Lee HE, Weitzel DH, Park K, Lee SH, Lee CT, Stephenson TN, Park H, Fitzgerald MC, Chi JT, Mook RA, Dewhirst MW, Lee YM, Hong J.
J Med Chem (2015) 58 : 7659 -7671
PubMed 26394152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.23 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2021442 MANASSANTIN A 1 7.96
CHEMBL3105545 1 6.50
CHEMBL3623807 1 6.46
CHEMBL3623808 1 6.42
CHEMBL3623806 1 6.37
CHEMBL3623812 1 6.23
CHEMBL3623811 1 6.16
CHEMBL3623805 1 6.04
CHEMBL3623810 1 5.84
CHEMBL3623809 1 5.71
CHEMBL3623803 1 5.68
CHEMBL3621232 1 5.43
CHEMBL3623804 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2021442 MANASSANTIN A IC50 = 11.0 nM 7.96
CHEMBL3105545 IC50 = 320.0 nM 6.50
CHEMBL3623807 IC50 = 350.0 nM 6.46
CHEMBL3623808 IC50 = 380.0 nM 6.42
CHEMBL3623806 IC50 = 430.0 nM 6.37
CHEMBL3623812 IC50 = 590.0 nM 6.23
CHEMBL3623811 IC50 = 690.0 nM 6.16
CHEMBL3623805 IC50 = 910.0 nM 6.04
CHEMBL3623810 IC50 = 1440.0 nM 5.84
CHEMBL3623809 IC50 = 1930.0 nM 5.71
CHEMBL3623803 IC50 = 2110.0 nM 5.68
CHEMBL3621232 IC50 = 3700.0 nM 5.43
CHEMBL3623804 IC50 > 10000000.0 nM -