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Assay Detail

CHEMBL5364262

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

Binding
Inhibition of N-terminal his6-tagged human recombinant AspH (315 to 758 residues) expressed in Escherichia coli BL21 (DE3) cells 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 5.46 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5429223 1 6.55
CHEMBL5415306 1 6.24
CHEMBL5429166 1 5.91
CHEMBL5423241 1 5.73
CHEMBL5414235 1 5.40
CHEMBL5401915 1 5.12
CHEMBL5438950 1 4.97
CHEMBL5414033 1 4.96
CHEMBL5397863 1 4.88
CHEMBL5409822 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5429223 IC50 = 280.0 nM 6.55
CHEMBL5415306 IC50 = 580.0 nM 6.24
CHEMBL5429166 IC50 = 1220.0 nM 5.91
CHEMBL5423241 IC50 = 1860.0 nM 5.73
CHEMBL5414235 IC50 = 3950.0 nM 5.40
CHEMBL5401915 IC50 = 7660.0 nM 5.12
CHEMBL5438950 IC50 = 10760.0 nM 4.97
CHEMBL5414033 IC50 = 10910.0 nM 4.96
CHEMBL5397863 IC50 = 13130.0 nM 4.88
CHEMBL5409822 IC50 = 16100.0 nM 4.79