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Assay Detail

CHEMBL5349109

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

Binding
Inhibition of recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE3) strain using H3K4me2 peptide as substrate incubated for 30 mins by fluorescence based analysis
37
Total Activities
37
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

Discovery of acridine-based LSD1 inhibitors as immune activators targeting LSD1 in gastric cancer.
Liu HM, Xiong XP, Wu JW, Chen HX, Zhou Y, Ji SK, Dai XJ, Zheng YC, Liu HM.
Eur J Med Chem (2023) 251 : 115255 -115255
PubMed 36913900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.19 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106525 1 7.14
CHEMBL5415964 1 7.07
CHEMBL5416497 1 7.00
CHEMBL217366 1 6.96
CHEMBL5404489 1 6.89
CHEMBL5419169 1 6.85
CHEMBL322748 1 6.66
CHEMBL5416205 1 6.64
CHEMBL5440680 1 6.64
CHEMBL5421422 1 6.55
CHEMBL5412335 1 6.35
CHEMBL289352 1 6.22
CHEMBL9806 1 6.18
CHEMBL5430017 1 6.16
CHEMBL5415883 1 6.15
CHEMBL5411051 1 6.13
CHEMBL5431065 1 6.07
CHEMBL43 AMSACRINE 4.0 1 6.06
CHEMBL1964647 1 6.01
CHEMBL49436 1 5.98
CHEMBL52101 1 5.94
CHEMBL5396199 1 5.78
CHEMBL5407377 1 5.76
CHEMBL5417480 1 5.62
CHEMBL22062 1 5.45
CHEMBL51599 1 5.44
CHEMBL5413825 1 5.41
CHEMBL5420365 1 5.22
CHEMBL433078 1 5.08
CHEMBL5437914 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106525 IC50 = 73.0 nM 7.14
CHEMBL5415964 IC50 = 85.0 nM 7.07
CHEMBL5416497 IC50 = 100.0 nM 7.00
CHEMBL217366 IC50 = 110.0 nM 6.96
CHEMBL5404489 IC50 = 130.0 nM 6.89
CHEMBL5419169 IC50 = 140.0 nM 6.85
CHEMBL322748 IC50 = 220.0 nM 6.66
CHEMBL5416205 IC50 = 230.0 nM 6.64
CHEMBL5440680 IC50 = 230.0 nM 6.64
CHEMBL5421422 IC50 = 280.0 nM 6.55
CHEMBL5412335 IC50 = 450.0 nM 6.35
CHEMBL289352 IC50 = 600.0 nM 6.22
CHEMBL9806 IC50 = 660.0 nM 6.18
CHEMBL5430017 IC50 = 700.0 nM 6.16
CHEMBL5415883 IC50 = 710.0 nM 6.15
CHEMBL5411051 IC50 = 740.0 nM 6.13
CHEMBL5431065 IC50 = 850.0 nM 6.07
CHEMBL43 AMSACRINE IC50 = 880.0 nM 6.06
CHEMBL1964647 IC50 = 970.0 nM 6.01
CHEMBL49436 IC50 = 1050.0 nM 5.98
CHEMBL52101 IC50 = 1160.0 nM 5.94
CHEMBL5396199 IC50 = 1660.0 nM 5.78
CHEMBL5407377 IC50 = 1720.0 nM 5.76
CHEMBL5417480 IC50 = 2390.0 nM 5.62
CHEMBL22062 IC50 = 3540.0 nM 5.45
CHEMBL51599 IC50 = 3620.0 nM 5.44
CHEMBL5413825 IC50 = 3860.0 nM 5.41
CHEMBL5420365 IC50 = 6030.0 nM 5.22
CHEMBL433078 IC50 = 8230.0 nM 5.08
CHEMBL5437914 IC50 - -
CHEMBL5432181 IC50 - -
CHEMBL5430268 IC50 - -
CHEMBL5420807 IC50 - -
CHEMBL48150 IC50 - -
CHEMBL5402084 IC50 - -
CHEMBL5440613 IC50 - -
CHEMBL295949 IC50 - -