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Assay Detail

CHEMBL5167390

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

Binding
Inhibition of N-terminal hexahistidine-SUMO-tagged human full length RIOK2 (residues 1 to 321) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins in presence of ATP by ADP-Glo 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

Serine/threonine-protein kinase RIO2 (CHEMBL6000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-<i>4H</i>-[1,2,3]triazolo[4,5-<i>c</i>]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor.
Ouyang Y, Si H, Zhu C, Zhong L, Ma H, Li Z, Xiong H, Liu T, Liu Z, Zhang Z, Zhang ZM, Cai Q.
J Med Chem (2022) 65 : 7833 -7842
PubMed 35584513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.86 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5172767 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5172767 IC50 = 139.0 nM 6.86