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Assay Detail

CHEMBL5364265

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

Binding
Inhibition of N-terminal his6-tagged AspH (315 to 758 residues) (unknown origin) expressed in Escherichia coli by SPE-MS analysis
10
Total Activities
10
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

Aspartyl/asparaginyl beta-hydroxylase (CHEMBL4680030)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Substituted Pyridine-2,4-dicarboxylate Derivatives Have Potential for Selective Inhibition of Human Jumonji-C Domain-Containing Protein 5.
Brewitz L, Nakashima Y, Piasecka SK, Salah E, Fletcher SC, Tumber A, Corner TP, Kennedy TJ, Fiorini G, Thalhammer A, Christensen KE, Coleman ML, Schofield CJ.
J Med Chem (2023) 66 : 10849 -10865
PubMed 37527664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.69 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425339 1 6.30
CHEMBL5428941 1 6.05
CHEMBL5407378 1 5.92
CHEMBL5434665 1 5.75
CHEMBL5419332 1 5.72
CHEMBL5396670 1 5.70
CHEMBL5423565 1 5.58
CHEMBL5402035 1 5.55
CHEMBL5408048 1 5.23
CHEMBL5408058 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425339 IC50 = 500.0 nM 6.30
CHEMBL5428941 IC50 = 900.0 nM 6.05
CHEMBL5407378 IC50 = 1200.0 nM 5.92
CHEMBL5434665 IC50 = 1800.0 nM 5.75
CHEMBL5419332 IC50 = 1900.0 nM 5.72
CHEMBL5396670 IC50 = 2000.0 nM 5.70
CHEMBL5423565 IC50 = 2600.0 nM 5.58
CHEMBL5402035 IC50 = 2800.0 nM 5.55
CHEMBL5408048 IC50 = 5900.0 nM 5.23
CHEMBL5408058 IC50 = 8900.0 nM 5.05