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Assay Detail

CHEMBL4180198

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

Binding
Inhibition of LSD1 (unknown origin)
21
Total Activities
21
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 tranylcypromine analogs with an acylhydrazone substituent as LSD1 inactivators: Design, synthesis and their biological evaluation.
Sun K, Peng JD, Suo FZ, Zhang T, Fu YD, Zheng YC, Liu HM.
Bioorg Med Chem Lett (2017) 27 : 5036 -5039
PubMed 29037950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.59 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4212776 1 7.58
CHEMBL4204049 1 7.04
CHEMBL4208387 1 6.96
CHEMBL4216474 1 6.83
CHEMBL4215722 1 6.77
CHEMBL4205178 1 6.70
CHEMBL4203790 1 6.65
CHEMBL4214175 1 6.65
CHEMBL4209901 1 6.65
CHEMBL4203515 1 6.60
CHEMBL4217387 1 6.56
CHEMBL4214864 1 6.56
CHEMBL4212293 1 6.46
CHEMBL4202897 1 6.46
CHEMBL4209645 1 6.44
CHEMBL4211184 1 6.41
CHEMBL4214311 1 6.37
CHEMBL4206303 1 6.34
CHEMBL4210623 1 6.20
CHEMBL4209568 1 6.08
CHEMBL4208534 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4212776 IC50 = 26.13 nM 7.58
CHEMBL4204049 IC50 = 91.83 nM 7.04
CHEMBL4208387 IC50 = 110.25 nM 6.96
CHEMBL4216474 IC50 = 147.7 nM 6.83
CHEMBL4215722 IC50 = 169.61 nM 6.77
CHEMBL4205178 IC50 = 201.23 nM 6.70
CHEMBL4203790 IC50 = 224.11 nM 6.65
CHEMBL4214175 IC50 = 221.97 nM 6.65
CHEMBL4209901 IC50 = 223.13 nM 6.65
CHEMBL4203515 IC50 = 253.6 nM 6.60
CHEMBL4217387 IC50 = 273.72 nM 6.56
CHEMBL4214864 IC50 = 273.83 nM 6.56
CHEMBL4212293 IC50 = 349.06 nM 6.46
CHEMBL4202897 IC50 = 350.26 nM 6.46
CHEMBL4209645 IC50 = 366.54 nM 6.44
CHEMBL4211184 IC50 = 388.08 nM 6.41
CHEMBL4214311 IC50 = 423.42 nM 6.37
CHEMBL4206303 IC50 = 455.51 nM 6.34
CHEMBL4210623 IC50 = 631.19 nM 6.20
CHEMBL4209568 IC50 = 828.31 nM 6.08
CHEMBL4208534 IC50 = 881.51 nM 6.05