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Assay Detail

CHEMBL981182

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

Binding
Inhibition of PKCbeta2
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Protein kinase C beta type (CHEMBL3045)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.
Hirabayashi A, Mukaiyama H, Kobayashi H, Shiohara H, Nakayama S, Ozawa M, Miyazawa K, Misawa K, Ohnota H, Isaji M.
Bioorg Med Chem (2008) 16 : 7347 -7357
PubMed 18585046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.72 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.40
CHEMBL475609 1 6.17
CHEMBL475575 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 4.0 nM 8.40
CHEMBL475609 IC50 = 680.0 nM 6.17
CHEMBL475575 IC50 = 2660.0 nM 5.58