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Assay Detail

CHEMBL4039114

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

Binding
Inhibition of recombinant human His-tagged LSD1 expressed in Escherichia coli BL21 (DE3) using H3K4me2 peptide as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by Amplex red dye based fluorescence assay
27
Total Activities
27
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

Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).
Borrello MT, Schinor B, Bartels K, Benelkebir H, Pereira S, Al-Jamal WT, Douglas L, Duriez PJ, Packham G, Haufe G, Ganesan A.
Bioorg Med Chem Lett (2017) 27 : 2099 -2101
PubMed 28390942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.38 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063580 1 6.10
CHEMBL4088366 1 5.92
CHEMBL468597 1 5.68
CHEMBL4083895 1 5.39
CHEMBL4098523 1 5.17
CHEMBL466770 1 5.17
CHEMBL4080504 1 5.17
CHEMBL4079589 1 5.09
CHEMBL4103844 1 5.08
CHEMBL4075414 1 5.04
CHEMBL4088315 1 -
CHEMBL4103002 1 -
CHEMBL4076750 1 -
CHEMBL4060129 1 -
CHEMBL4061133 1 -
CHEMBL4083013 1 -
CHEMBL4090801 1 -
CHEMBL4104945 1 -
CHEMBL4087091 1 -
CHEMBL469024 1 -
CHEMBL455782 1 -
CHEMBL468852 1 -
CHEMBL462630 1 -
CHEMBL447729 1 -
CHEMBL4083630 1 -
CHEMBL4074238 1 -
CHEMBL4069807 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063580 IC50 = 800.0 nM 6.10
CHEMBL4088366 IC50 = 1200.0 nM 5.92
CHEMBL468597 IC50 = 2100.0 nM 5.68
CHEMBL4083895 IC50 = 4100.0 nM 5.39
CHEMBL4098523 IC50 = 6800.0 nM 5.17
CHEMBL466770 IC50 = 6700.0 nM 5.17
CHEMBL4080504 IC50 = 6700.0 nM 5.17
CHEMBL4079589 IC50 = 8200.0 nM 5.09
CHEMBL4103844 IC50 = 8400.0 nM 5.08
CHEMBL4075414 IC50 = 9200.0 nM 5.04
CHEMBL4088315 IC50 > 50000.0 nM -
CHEMBL4103002 IC50 > 50000.0 nM -
CHEMBL4076750 IC50 > 50000.0 nM -
CHEMBL4060129 IC50 > 25000.0 nM -
CHEMBL4061133 IC50 > 25000.0 nM -
CHEMBL4083013 IC50 > 25000.0 nM -
CHEMBL4090801 IC50 > 50000.0 nM -
CHEMBL4104945 IC50 > 25000.0 nM -
CHEMBL4087091 IC50 > 25000.0 nM -
CHEMBL469024 IC50 > 25000.0 nM -
CHEMBL455782 IC50 > 25000.0 nM -
CHEMBL468852 IC50 > 25000.0 nM -
CHEMBL462630 IC50 > 25000.0 nM -
CHEMBL447729 IC50 > 25000.0 nM -
CHEMBL4083630 IC50 > 50000.0 nM -
CHEMBL4074238 IC50 > 50000.0 nM -
CHEMBL4069807 IC50 > 50000.0 nM -