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Assay Detail

CHEMBL4024496

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

Binding
Binding affinity to ARID/PHD1/Zn binding domain truncated human N-terminal His-SUMO-tagged KDM5A (1 to 588 residues) expressed in Escherichia coli by ITC
12
Total Activities
12
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

Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X.
J Med Chem (2018) 61 : 3193 -3208
PubMed 29537847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 6.45 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4096760 1 7.22
CHEMBL4081571 1 6.82
CHEMBL4090351 1 6.75
CHEMBL4070992 1 6.68
CHEMBL4062359 1 6.66
CHEMBL4066179 1 6.60
CHEMBL4077310 1 6.39
CHEMBL4059617 1 6.33
CHEMBL4100530 1 6.28
CHEMBL4088737 1 5.62
CHEMBL4078388 1 5.57
CHEMBL4067490 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4096760 Kd = 60.0 nM 7.22
CHEMBL4081571 Kd = 150.0 nM 6.82
CHEMBL4090351 Kd = 180.0 nM 6.75
CHEMBL4070992 Kd = 210.0 nM 6.68
CHEMBL4062359 Kd = 220.0 nM 6.66
CHEMBL4066179 Kd = 250.0 nM 6.60
CHEMBL4077310 Kd = 410.0 nM 6.39
CHEMBL4059617 Kd = 470.0 nM 6.33
CHEMBL4100530 Kd = 530.0 nM 6.28
CHEMBL4088737 Kd = 2400.0 nM 5.62
CHEMBL4078388 Kd = 2700.0 nM 5.57
CHEMBL4067490 Kd > 12000.0 nM -