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Assay Detail

CHEMBL1798563

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

Binding
Inhibition of LSD1
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Lysine-specific histone demethylase 1A (CHEMBL6136)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of histone demethylases.
Lohse B, Kristensen JL, Kristensen LH, Agger K, Helin K, Gajhede M, Clausen RP.
Bioorg Med Chem (2011) 19 : 3625 -3636
PubMed 21596573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.95 7.30
IC50 5 5.31 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1797647 1 7.30
CHEMBL1795980 1 6.21
CHEMBL1797651 1 6.16
CHEMBL1797650 1 6.05
CHEMBL1795981 1 6.00
CHEMBL1797640 1 6.00
CHEMBL1797641 1 6.00
CHEMBL1797645 1 5.82
CHEMBL1797646 1 5.75
CHEMBL1215658 1 5.70
CHEMBL1797639 1 5.70
CHEMBL1797652 1 5.36
CHEMBL1797642 1 5.05
CHEMBL1797643 1 5.05
CHEMBL1797644 1 5.05
CHEMBL1089 PHENELZINE 4.0 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1797647 Ki = 50.0 nM 7.30
CHEMBL1795980 Ki = 610.0 nM 6.21
CHEMBL1797651 Ki = 700.0 nM 6.16
CHEMBL1797650 Ki = 900.0 nM 6.05
CHEMBL1795981 Ki = 1000.0 nM 6.00
CHEMBL1797640 Ki = 1000.0 nM 6.00
CHEMBL1797641 Ki = 1000.0 nM 6.00
CHEMBL1797645 Ki = 1500.0 nM 5.82
CHEMBL1797646 Ki = 1800.0 nM 5.75
CHEMBL1215658 IC50 = 2000.0 nM 5.70
CHEMBL1797639 IC50 = 2000.0 nM 5.70
CHEMBL1797652 Ki = 4400.0 nM 5.36
CHEMBL1797642 IC50 = 9000.0 nM 5.05
CHEMBL1797643 IC50 = 9000.0 nM 5.05
CHEMBL1797644 IC50 = 9000.0 nM 5.05
CHEMBL1089 PHENELZINE Ki = 17600.0 nM 4.75