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Assay Detail

CHEMBL3624714

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Binding
Inhibition of KDM6B (unknown origin)
6
Total Activities
6
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

Lysine-specific demethylase 6B (CHEMBL1938211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
England KS, Tumber A, Krojer T, Scozzafava G, Ng SS, Daniel M, Szykowska A, Che K, von Delft F, Burgess-Brown NA, Kawamura A, Schofield CJ, Brennan PE.
Medchemcomm (2014) 5 : 1879 -1886
PubMed 26682034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.95 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3188597 1 7.20
CHEMBL1230640 1 7.00
CHEMBL90852 N-OXALYLGLYCINE 1 6.50
CHEMBL1982368 1 6.10
CHEMBL316034 1 4.50
CHEMBL3621850 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3188597 IC50 = 63.1 nM 7.20
CHEMBL1230640 IC50 = 100.0 nM 7.00
CHEMBL90852 N-OXALYLGLYCINE IC50 = 316.23 nM 6.50
CHEMBL1982368 IC50 = 794.33 nM 6.10
CHEMBL316034 IC50 = 31622.78 nM 4.50
CHEMBL3621850 IC50 = 39810.72 nM 4.40