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Assay Detail

CHEMBL5127922

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Binding
Inhibition of full-length recombinant KDM1A (unknown origin) expressed in Escherichia coli BL21 DE using H3K4Me2 peptide as substrate incubated for 0.5 hrs by Amplex red assay
3
Total Activities
3
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 3 6.32 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3401107 1 6.74
CHEMBL3330503 1 6.39
CHEMBL19344 HIGENAMINE 1.0 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3401107 IC50 = 183.0 nM 6.74
CHEMBL3330503 IC50 = 407.0 nM 6.39
CHEMBL19344 HIGENAMINE IC50 = 1470.0 nM 5.83