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Assay Detail

CHEMBL4427933

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

Binding
Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/20 uM 2-OG as substrate/co-factor by TR-FRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysine-specific demethylase 5A (CHEMBL2424504)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent, selective KDM5 inhibitors.
Gehling VS, Bellon SF, Harmange JC, LeBlanc Y, Poy F, Odate S, Buker S, Lan F, Arora S, Williamson KE, Sandy P, Cummings RT, Bailey CM, Bergeron L, Mao W, Gustafson A, Liu Y, VanderPorten E, Audia JE, Trojer P, Albrecht BK.
Bioorg Med Chem Lett (2016) 26 : 4350 -4354
PubMed 27476424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454253 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454253 IC50 = 20.0 nM 7.70