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Assay Detail

CHEMBL4358946

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

Binding
Competitive inhibition of human N-terminal His6-tagged TEV protease site linked DHPS expressed in Escherichia coli BL21 (DE3) assessed as reduction in radiolabelled amino-butylidene incorporation in eIF5A using 2 uM of [3H]Spermidine trichloride as substrate after 90 to 120 mins in presence of eIF5A and 250 uM NAD+ by Topcount scintillation counting method
3
Total Activities
3
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

Deoxyhypusine synthase (CHEMBL4415)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.
Tanaka Y, Kurasawa O, Yokota A, Klein MG, Ono K, Saito B, Matsumoto S, Okaniwa M, Ambrus-Aikelin G, Morishita D, Kitazawa S, Uchiyama N, Ogawa K, Kimura H, Imamura S.
J Med Chem (2020) 63 : 3215 -3226
PubMed 32142284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.99 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229457 1 6.30
CHEMBL4447948 1 4.42
CHEMBL4555677 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229457 IC50 = 500.0 nM 6.30
CHEMBL4447948 IC50 = 38000.0 nM 4.42
CHEMBL4555677 IC50 = 56000.0 nM 4.25