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Assay Detail

CHEMBL3772964

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

Binding
Inhibition of KDM4A (unknown origin) by RFMS assay
7
Total Activities
7
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 4A (CHEMBL5896)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Drewes G, Eagle R, Garton N, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Pemberton M, Rioja I, Seal GA, Shipley T, Singh O, Suckling CJ, Taylor J, Thomas P, Wilson DM, Lee K, Prinjha RK.
J Med Chem (2016) 59 : 1370 -1387
PubMed 26771203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.17 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770740 1 6.40
CHEMBL1383671 1 6.30
CHEMBL3771180 1 6.20
CHEMBL3771198 1 6.20
CHEMBL3769724 1 6.10
CHEMBL3769511 1 5.80
CHEMBL3770732 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770740 IC50 = 398.11 nM 6.40
CHEMBL1383671 IC50 = 501.19 nM 6.30
CHEMBL3771180 IC50 = 630.96 nM 6.20
CHEMBL3771198 IC50 = 630.96 nM 6.20
CHEMBL3769724 IC50 = 794.33 nM 6.10
CHEMBL3769511 IC50 = 1584.89 nM 5.80
CHEMBL3770732 IC50 > 100000.0 nM -