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Assay Detail

CHEMBL4682230

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Binding
Binding affinity to human Vps34 expressed in mammalian expression system
4
Total Activities
4
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
Kd 4 8.54 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2140173 1 8.77
CHEMBL4794132 1 8.70
CHEMBL4752634 1 8.40
CHEMBL4792737 1 8.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2140173 Kd = 1.7 nM 8.77
CHEMBL4794132 Kd = 2.0 nM 8.70
CHEMBL4752634 Kd = 4.0 nM 8.40
CHEMBL4792737 Kd = 5.1 nM 8.29