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Assay Detail

CHEMBL5159713

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

Binding
Inhibition of recombinant human full length LSD2 using biotinylated H3K4Me2 peptide as substrate by TR-FRET assay
24
Total Activities
24
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 2 (CHEMBL1938208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Li C, Su M, Zhu W, Kan W, Ge T, Xu G, Wang S, Sheng L, Gao F, Ye Y, Wang J, Zhou Y, Li J, Liu H.
J Med Chem (2022) 65 : 4335 -4349
PubMed 35200034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.45 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5206450 1 6.22
CHEMBL5191047 1 6.12
CHEMBL5205837 1 6.10
CHEMBL5181753 1 6.00
CHEMBL5196564 1 5.99
CHEMBL5177857 1 5.83
CHEMBL5194745 1 5.65
CHEMBL5184995 1 5.59
CHEMBL5170567 1 5.49
CHEMBL5204790 1 5.40
CHEMBL5172252 1 5.40
CHEMBL5174650 1 5.40
CHEMBL5191876 1 5.38
CHEMBL5201504 1 5.35
CHEMBL5170011 1 5.30
CHEMBL5208082 1 5.27
CHEMBL5175125 1 5.19
CHEMBL5197243 1 5.12
CHEMBL5171190 1 5.05
CHEMBL5191605 1 5.04
CHEMBL5183291 1 5.01
CHEMBL5196436 1 4.81
CHEMBL5174599 1 4.71
CHEMBL3786182 GSK2879552 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5206450 IC50 = 600.0 nM 6.22
CHEMBL5191047 IC50 = 760.0 nM 6.12
CHEMBL5205837 IC50 = 800.0 nM 6.10
CHEMBL5181753 IC50 = 1010.0 nM 6.00
CHEMBL5196564 IC50 = 1020.0 nM 5.99
CHEMBL5177857 IC50 = 1480.0 nM 5.83
CHEMBL5194745 IC50 = 2260.0 nM 5.65
CHEMBL5184995 IC50 = 2550.0 nM 5.59
CHEMBL5170567 IC50 = 3260.0 nM 5.49
CHEMBL5204790 IC50 = 4000.0 nM 5.40
CHEMBL5172252 IC50 = 4000.0 nM 5.40
CHEMBL5174650 IC50 = 3950.0 nM 5.40
CHEMBL5191876 IC50 = 4120.0 nM 5.38
CHEMBL5201504 IC50 = 4510.0 nM 5.35
CHEMBL5170011 IC50 = 5000.0 nM 5.30
CHEMBL5208082 IC50 = 5420.0 nM 5.27
CHEMBL5175125 IC50 = 6470.0 nM 5.19
CHEMBL5197243 IC50 = 7510.0 nM 5.12
CHEMBL5171190 IC50 = 8890.0 nM 5.05
CHEMBL5191605 IC50 = 9130.0 nM 5.04
CHEMBL5183291 IC50 = 9800.0 nM 5.01
CHEMBL5196436 IC50 = 15560.0 nM 4.81
CHEMBL5174599 IC50 = 19510.0 nM 4.71
CHEMBL3786182 GSK2879552 IC50 > 100000.0 nM -