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Assay Detail

CHEMBL4270048

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

Binding
Binding affinity to KDM5A ARID/PhD1 domain deletion mutant (1 to 588 residues) (unknown origin) by ITC assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X.
J Med Chem (2018) 61 : 10588 -10601
PubMed 30392349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 5.72 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081571 1 6.82
CHEMBL4284220 1 6.58
CHEMBL4283844 1 5.22
CHEMBL4294426 1 5.05
CHEMBL3188597 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081571 Kd = 150.0 nM 6.82
CHEMBL4284220 Kd = 260.0 nM 6.58
CHEMBL4283844 Kd = 6000.0 nM 5.22
CHEMBL4294426 Kd = 9000.0 nM 5.05
CHEMBL3188597 Kd = 12000.0 nM 4.92