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Assay Detail

CHEMBL5364264

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

Binding
Inhibition of N-terminal his6-tagged FIH (unknown origin) expressed in Escherichia coli using HIF-alpha CAD (788 to 822 residues) 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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4.58 5.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5423565 1 5.01
CHEMBL5425339 1 4.61
CHEMBL5419332 1 4.59
CHEMBL5407378 1 4.54
CHEMBL5402035 1 4.53
CHEMBL5408048 1 4.50
CHEMBL5396670 1 4.50
CHEMBL5434665 1 4.47
CHEMBL5428941 1 4.44
CHEMBL5408058 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5423565 IC50 = 9700.0 nM 5.01
CHEMBL5425339 IC50 = 24300.0 nM 4.61
CHEMBL5419332 IC50 = 25600.0 nM 4.59
CHEMBL5407378 IC50 = 28800.0 nM 4.54
CHEMBL5402035 IC50 = 29700.0 nM 4.53
CHEMBL5408048 IC50 = 31900.0 nM 4.50
CHEMBL5396670 IC50 = 31700.0 nM 4.50
CHEMBL5434665 IC50 = 33600.0 nM 4.47
CHEMBL5428941 IC50 = 36300.0 nM 4.44
CHEMBL5408058 IC50 > 50000.0 nM -