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Assay Detail

CHEMBL686884

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

Functional
Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct 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 6 7.29 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103055 1 7.60
CHEMBL321315 1 7.35
CHEMBL106384 1 7.34
CHEMBL321529 1 7.24
CHEMBL388978 STAUROSPORINE 1 7.11
CHEMBL103628 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103055 IC50 = 25.0 nM 7.60
CHEMBL321315 IC50 = 45.0 nM 7.35
CHEMBL106384 IC50 = 46.0 nM 7.34
CHEMBL321529 IC50 = 58.0 nM 7.24
CHEMBL388978 STAUROSPORINE IC50 = 77.0 nM 7.11
CHEMBL103628 IC50 = 82.0 nM 7.09