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Assay Detail

CHEMBL5524261

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

Binding
Inhibition of recombinant human KDM5B (1 to 822 residues) expressed in baculovirus infected Sf9 cells using histone H3 peptide and L-ascorbic acid as substrate preincubated for 15 mins followed by substrate and 2-OG addition measured after 60 mins by Alphascreen assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysine-specific demethylase 5B (CHEMBL3774295)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling.
Šimelis K, Saraç H, Salah E, Nishio K, McAllister TE, Corner TP, Tumber A, Belle R, Schofield CJ, Suga H, Kawamura A.
Bioorg Med Chem (2024) 99 : 117597 -117597
PubMed 38262305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pIC50 2 - -
IC50 1 4.63 4.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557372 1 4.63
CHEMBL1230640 1 -
CHEMBL5542589 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557372 IC50 = 23442.29 nM 4.63
CHEMBL1230640 pIC50 - -
CHEMBL5542589 pIC50 - -