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Assay Detail

CHEMBL4008771

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

Binding
Competitive inhibition of recombinant human KDM1A/CoREST complex expressed in Escherichia coli using H3K4me1 peptide as substrate preincubated for 15 mins followed by substrate addition measured for 12 mins by Lineweaver-Burk plot analysis
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

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration.
Sartori L, Mercurio C, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Vultaggio S, Botrugno OA, Dessanti P, Minucci S, Zagarrí E, Carettoni D, Iuzzolino L, Varasi M, Vianello P.
J Med Chem (2017) 60 : 1673 -1692
PubMed 28186755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 4.32 4.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086085 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086085 Ki = 48400.0 nM 4.32