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Assay Detail

CHEMBL5584869

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

Binding
Inhibition of recombinant human KDM5B (M1 to R822 residues) expressed in Sf9 cells using 2-OG and histone H3 substrate peptide as substrates preincubated for 15 mins followed by substrate addition and measured after 20 mins by AlphaScreen assay
1
Total Activities
1
Compounds Tested
1
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

Discovery of an efficacious KDM5B PROTAC degrader GT-653 up-regulating IFN response genes in prostate cancer.
Guan T, Zhang Y, Li S, Zhang W, Song Y, Li Y, He Y, Chen Y.
Eur J Med Chem (2024) 272 : 116494 -116494
PubMed 38749268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3787669 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3787669 IC50 = 4.0 nM 8.40