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Assay Detail

CHEMBL4826336

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

Binding
Inhibition of human recombinant LSD1 by horseradish peroxidase-coupled fluorometric assay
40
Total Activities
40
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

Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors.
Zhang X, Huang H, Zhang Z, Yan J, Wu T, Yin W, Sun Y, Wang X, Gu Y, Zhao D, Cheng M.
Eur J Med Chem (2021) 220 : 113501 -113501
PubMed 33945992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.59 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854446 1 7.28
CHEMBL4856172 1 7.21
CHEMBL4863608 1 7.21
CHEMBL4858199 1 7.19
CHEMBL4873407 1 7.13
CHEMBL4857710 1 7.12
CHEMBL4867217 1 7.05
CHEMBL4862184 1 6.97
CHEMBL4875708 1 6.94
CHEMBL4862965 1 6.91
CHEMBL4867394 1 6.89
CHEMBL4864707 1 6.89
CHEMBL4848676 1 6.87
CHEMBL3759201 1 6.87
CHEMBL4862640 1 6.87
CHEMBL4875303 1 6.84
CHEMBL4860041 1 6.83
CHEMBL4878035 1 6.81
CHEMBL4869351 1 6.80
CHEMBL4870715 1 6.77
CHEMBL4858064 1 6.76
CHEMBL4878624 1 6.74
CHEMBL4864665 1 6.73
CHEMBL4874220 1 6.66
CHEMBL4851421 1 6.66
CHEMBL4867816 1 6.65
CHEMBL4876005 1 6.64
CHEMBL4874997 1 6.60
CHEMBL4874246 1 6.57
CHEMBL4868387 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854446 IC50 = 53.0 nM 7.28
CHEMBL4856172 IC50 = 61.0 nM 7.21
CHEMBL4863608 IC50 = 61.0 nM 7.21
CHEMBL4858199 IC50 = 64.0 nM 7.19
CHEMBL4873407 IC50 = 74.0 nM 7.13
CHEMBL4857710 IC50 = 76.0 nM 7.12
CHEMBL4867217 IC50 = 90.0 nM 7.05
CHEMBL4862184 IC50 = 108.0 nM 6.97
CHEMBL4875708 IC50 = 114.0 nM 6.94
CHEMBL4862965 IC50 = 122.0 nM 6.91
CHEMBL4864707 IC50 = 128.0 nM 6.89
CHEMBL4867394 IC50 = 128.0 nM 6.89
CHEMBL4848676 IC50 = 135.0 nM 6.87
CHEMBL3759201 IC50 = 134.0 nM 6.87
CHEMBL4862640 IC50 = 135.0 nM 6.87
CHEMBL4875303 IC50 = 145.0 nM 6.84
CHEMBL4860041 IC50 = 147.0 nM 6.83
CHEMBL4878035 IC50 = 154.0 nM 6.81
CHEMBL4869351 IC50 = 158.0 nM 6.80
CHEMBL4870715 IC50 = 170.0 nM 6.77
CHEMBL4858064 IC50 = 172.0 nM 6.76
CHEMBL4878624 IC50 = 184.0 nM 6.74
CHEMBL4864665 IC50 = 188.0 nM 6.73
CHEMBL4874220 IC50 = 220.0 nM 6.66
CHEMBL4851421 IC50 = 221.0 nM 6.66
CHEMBL4867816 IC50 = 225.0 nM 6.65
CHEMBL4876005 IC50 = 229.0 nM 6.64
CHEMBL4874997 IC50 = 252.0 nM 6.60
CHEMBL4874246 IC50 = 267.0 nM 6.57
CHEMBL4868387 IC50 = 408.0 nM 6.39
CHEMBL4852701 IC50 = 415.0 nM 6.38
CHEMBL4851170 IC50 = 420.0 nM 6.38
CHEMBL4871199 IC50 = 500.0 nM 6.30
CHEMBL4846305 IC50 = 674.0 nM 6.17
CHEMBL4876002 IC50 = 730.0 nM 6.14
CHEMBL4872237 IC50 = 1484.0 nM 5.83
CHEMBL4846793 IC50 = 2096.0 nM 5.68
CHEMBL4874983 IC50 = 2616.0 nM 5.58
CHEMBL4857917 IC50 = 9193.0 nM 5.04
CHEMBL4289507 IC50 = 40500.0 nM 4.39