Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5123804

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

Binding
Inhibition of human LSD1/CoREST using histone H3 peptide as substrate by fluorescence polarization assay
13
Total Activities
13
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

Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.
Menna M, Fiorentino F, Marrocco B, Lucidi A, Tomassi S, Cilli D, Romanenghi M, Cassandri M, Pomella S, Pezzella M, Del Bufalo D, Zeya Ansari MS, Tomašević N, Mladenović M, Viviano M, Sbardella G, Rota R, Trisciuoglio D, Minucci S, Mattevi A, Rotili D, Mai A.
Eur J Med Chem (2022) 237 : 114410 -114410
PubMed 35525212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.77 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3134377 1 7.46
CHEMBL5202637 1 6.97
CHEMBL5170197 1 6.84
CHEMBL5179091 1 6.83
CHEMBL5198334 1 6.82
CHEMBL5178765 1 6.81
CHEMBL5175171 1 6.77
CHEMBL5186174 1 6.76
CHEMBL5181017 1 6.74
CHEMBL5205888 1 6.69
CHEMBL5204694 1 6.67
CHEMBL1232432 1 6.36
CHEMBL5189687 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3134377 Ki = 35.0 nM 7.46
CHEMBL5202637 Ki = 108.0 nM 6.97
CHEMBL5170197 Ki = 146.0 nM 6.84
CHEMBL5179091 Ki = 149.0 nM 6.83
CHEMBL5198334 Ki = 153.0 nM 6.82
CHEMBL5178765 Ki = 156.0 nM 6.81
CHEMBL5175171 Ki = 170.0 nM 6.77
CHEMBL5186174 Ki = 175.0 nM 6.76
CHEMBL5181017 Ki = 183.0 nM 6.74
CHEMBL5205888 Ki = 205.0 nM 6.69
CHEMBL5204694 Ki = 212.0 nM 6.67
CHEMBL1232432 Ki = 440.0 nM 6.36
CHEMBL5189687 Ki = 569.0 nM 6.25