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Assay Detail

CHEMBL4682233

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

Binding
Inhibition of recombinant full-length human VPS34 incubated for 60 mins by ADP-Glo kinase 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

Publication

Optimization of Potent and Selective Ataxia Telangiectasia-Mutated Inhibitors Suitable for a Proof-of-Concept Study in Huntington's Disease Models.
Toledo-Sherman L,Breccia P,Cachope R,Bate JR,Angulo-Herrera I,Wishart G,Matthews KL,Martin SL,Cox HC,McAllister G,Penrose SD,Vater H,Esmieu W,Van de Poël A,Van de Bospoort R,Strijbosch A,Lamers M,Leonard P,Jarvis RE,Blackaby W,Barnes K,Eznarriaga M,Dowler S,Smith GD,Fischer DF,Lazari O,Yates D,Rose M,Jang SW,Muñoz-Sanjuan I,Dominguez C
J Med Chem (2019) 62 : 2988 -3008
PubMed 30840447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.58 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4745255 1 7.85
CHEMBL2140173 1 7.77
CHEMBL4760480 1 7.70
CHEMBL4794132 1 7.62
CHEMBL4792737 1 7.54
CHEMBL4752634 1 7.39
CHEMBL4783168 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4745255 IC50 = 14.0 nM 7.85
CHEMBL2140173 IC50 = 17.0 nM 7.77
CHEMBL4760480 IC50 = 20.0 nM 7.70
CHEMBL4794132 IC50 = 24.0 nM 7.62
CHEMBL4792737 IC50 = 29.0 nM 7.54
CHEMBL4752634 IC50 = 41.0 nM 7.39
CHEMBL4783168 IC50 = 67.0 nM 7.17