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Assay Detail

CHEMBL4310494

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

Binding
Inhibition of LSD1 in human THP1 cells assessed as induction of CD11b expression after 4 days by LIVE/DEAD violet staining based FACS analysis
25
Total Activities
25
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

Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors.
Nie Z, Shi L, Lai C, Severin C, Xu J, Del Rosario JR, Stansfield RK, Cho RW, Kanouni T, Veal JM, Stafford JA, Chen YK.
Bioorg Med Chem Lett (2019) 29 : 103 -106
PubMed 30409536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 7.29 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4522607 1 8.10
CHEMBL4451607 1 7.89
CHEMBL4444902 1 7.85
CHEMBL4451430 1 7.66
CHEMBL4447527 1 7.60
CHEMBL4548929 1 7.58
CHEMBL4448358 1 7.57
CHEMBL4454128 1 7.47
CHEMBL4514358 1 7.37
CHEMBL4517147 1 7.35
CHEMBL4537429 1 7.33
CHEMBL4453520 1 7.30
CHEMBL4569059 1 7.23
CHEMBL4465367 1 7.23
CHEMBL3134377 1 7.21
CHEMBL4440004 1 7.18
CHEMBL4516248 1 7.17
CHEMBL4440870 1 7.04
CHEMBL4437380 1 7.00
CHEMBL4581929 1 6.96
CHEMBL4530322 1 6.96
CHEMBL4591673 1 6.85
CHEMBL4437892 1 6.85
CHEMBL4527219 1 6.82
CHEMBL4560537 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4522607 EC50 = 8.0 nM 8.10
CHEMBL4451607 EC50 = 13.0 nM 7.89
CHEMBL4444902 EC50 = 14.0 nM 7.85
CHEMBL4451430 EC50 = 22.0 nM 7.66
CHEMBL4447527 EC50 = 25.0 nM 7.60
CHEMBL4548929 EC50 = 26.0 nM 7.58
CHEMBL4448358 EC50 = 27.0 nM 7.57
CHEMBL4454128 EC50 = 34.0 nM 7.47
CHEMBL4514358 EC50 = 43.0 nM 7.37
CHEMBL4517147 EC50 = 45.0 nM 7.35
CHEMBL4537429 EC50 = 47.0 nM 7.33
CHEMBL4453520 EC50 = 50.0 nM 7.30
CHEMBL4569059 EC50 = 59.0 nM 7.23
CHEMBL4465367 EC50 = 59.0 nM 7.23
CHEMBL3134377 EC50 = 62.0 nM 7.21
CHEMBL4440004 EC50 = 66.0 nM 7.18
CHEMBL4516248 EC50 = 68.0 nM 7.17
CHEMBL4440870 EC50 = 92.0 nM 7.04
CHEMBL4437380 EC50 = 100.0 nM 7.00
CHEMBL4581929 EC50 = 110.0 nM 6.96
CHEMBL4530322 EC50 = 110.0 nM 6.96
CHEMBL4591673 EC50 = 140.0 nM 6.85
CHEMBL4437892 EC50 = 140.0 nM 6.85
CHEMBL4527219 EC50 = 150.0 nM 6.82
CHEMBL4560537 EC50 = 160.0 nM 6.80