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Assay Detail

CHEMBL4031661

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

Binding
Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by HRE dual-luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.
Naik R, Ban HS, Jang K, Kim I, Xu X, Harmalkar D, Shin SA, Kim M, Kim BK, Park J, Ku B, Oh S, Won M, Lee K.
J Med Chem (2017) 60 : 8631 -8646
PubMed 28991459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.98 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178407 1 6.13
CHEMBL4068781 1 5.97
CHEMBL4091027 1 5.85
CHEMBL4068233 1 -
CHEMBL4085170 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178407 IC50 = 740.0 nM 6.13
CHEMBL4068781 IC50 = 1080.0 nM 5.97
CHEMBL4091027 IC50 = 1400.0 nM 5.85
CHEMBL4068233 IC50 > 40000.0 nM -
CHEMBL4085170 IC50 > 40000.0 nM -