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Assay Detail

CHEMBL768280

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Binding
Inhibition of Protein kinase C beta 2
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.
Zhang HC, White KB, Ye H, McComsey DF, Derian CK, Addo MF, Andrade-Gordon P, Eckardt AJ, Conway BR, Westover L, Xu JZ, Look R, Demarest KT, Emanuel S, Maryanoff BE.
Bioorg Med Chem Lett (2003) 13 : 3049 -3053
PubMed 12941331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.50 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106384 1 8.05
CHEMBL103055 1 8.05
CHEMBL388978 STAUROSPORINE 1 8.00
CHEMBL421217 1 7.77
CHEMBL103506 1 7.72
CHEMBL103628 1 7.57
CHEMBL321529 1 7.40
CHEMBL105477 1 7.39
CHEMBL106061 1 7.39
CHEMBL321315 1 7.34
CHEMBL105620 1 7.12
CHEMBL103421 1 6.96
CHEMBL319265 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106384 IC50 = 9.0 nM 8.05
CHEMBL103055 IC50 = 9.0 nM 8.05
CHEMBL388978 STAUROSPORINE IC50 = 10.0 nM 8.00
CHEMBL421217 IC50 = 17.0 nM 7.77
CHEMBL103506 IC50 = 19.0 nM 7.72
CHEMBL103628 IC50 = 27.0 nM 7.57
CHEMBL321529 IC50 = 40.0 nM 7.40
CHEMBL105477 IC50 = 41.0 nM 7.39
CHEMBL106061 IC50 = 41.0 nM 7.39
CHEMBL321315 IC50 = 46.0 nM 7.34
CHEMBL105620 IC50 = 75.0 nM 7.12
CHEMBL103421 IC50 = 110.0 nM 6.96
CHEMBL319265 IC50 = 200.0 nM 6.70