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Assay Detail

CHEMBL4814433

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

Binding
Inhibition of N-terminal His-SUMO tagged human LSD1 (172 to 852 residues)/His-tagged CoREST (286 to 482 residues) expressed in Escherichia coli BL21 (DE3) using ART(mK)QTARKSTGGKAPRKQLAGGK-Biotin as substrate preincubated for 60 mins followed by substrate addition and measured after 15 mins by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

LSD1/CoREST complex (CHEMBL3137262)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective.
Dai XJ, Liu Y, Xiong XP, Xue LP, Zheng YC, Liu HM.
J Med Chem (2020) 63 : 14197 -14215
PubMed 32931269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.68 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875015 1 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875015 IC50 = 2.1 nM 8.68