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Assay Detail

CHEMBL4407367

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Binding
Inhibition of PKC (unknown origin)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein kinase C (PKC) (CHEMBL2093867)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Dong X, Zhan W, Zhao M, Che J, Dai X, Wu Y, Xu L, Zhou Y, Zhao Y, Tian T, Cheng G, Jin Z, Li J, Shao Y, He Q, Yang B, Weng Q, Hu Y.
J Med Chem (2019) 62 : 7264 -7288
PubMed 31298542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.94 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4441825 1 7.80
CHEMBL4440965 1 7.03
CHEMBL4457064 1 6.81
CHEMBL3137336 UPROSERTIB 2.0 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4441825 IC50 = 16.0 nM 7.80
CHEMBL4440965 IC50 = 94.0 nM 7.03
CHEMBL4457064 IC50 = 156.0 nM 6.81
CHEMBL3137336 UPROSERTIB IC50 = 753.0 nM 6.12