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Assay Detail

CHEMBL4008767

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

Binding
Inhibition of recombinant human KDM1A/CoREST complex expressed in Escherichia coli using H3K4me1 peptide as substrate preincubated for 15 mins with enzyme followed by substrate addition measured after 12 mins by Amplex Ultra Red reagent based HRP enzyme coupled assay
3
Total Activities
3
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
IC50 3 4.39 4.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066708 1 4.57
CHEMBL3989843 TRANYLCYPROMINE 4.0 1 4.51
CHEMBL4086085 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066708 IC50 = 27100.0 nM 4.57
CHEMBL3989843 TRANYLCYPROMINE IC50 = 30600.0 nM 4.51
CHEMBL4086085 IC50 = 82400.0 nM 4.08