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Assay Detail

CHEMBL5127932

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Binding
Inhibition of recombinant human KDM1A (158 to 852 residues) using H3K4Me2 peptide as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by AlphaLISA assay
2
Total Activities
2
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 histone demethylase 1A (CHEMBL6136)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
He X, Zhang H, Zhang Y, Ye Y, Wang S, Bai R, Xie T, Ye XY.
Eur J Med Chem (2022) 231 : 114143 -114143
PubMed 35101649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.76 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4090812 1 8.11
CHEMBL5187087 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4090812 IC50 = 7.8 nM 8.11
CHEMBL5187087 IC50 = 4000.0 nM 5.40