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Assay Detail

CHEMBL2156012

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

Binding
Inhibition of PKCbeta-1 by scintillation proximity assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Wagner J, von Matt P, Faller B, Cooke NG, Albert R, Sedrani R, Wiegand H, Jean C, Beerli C, Weckbecker G, Evenou JP, Zenke G, Cottens S.
J Med Chem (2011) 54 : 6028 -6039
PubMed 21797275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.24 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151411 1 9.70
CHEMBL1996510 1 9.22
CHEMBL2153750 1 8.92
CHEMBL2151415 1 8.85
CHEMBL568580 1 8.74
CHEMBL565612 SOTRASTAURIN 2.0 1 8.70
CHEMBL2153748 1 8.70
CHEMBL2153749 1 8.42
CHEMBL2153755 1 8.30
CHEMBL2151412 1 8.29
CHEMBL2153747 1 8.28
CHEMBL2151410 1 8.22
CHEMBL2151408 1 8.19
CHEMBL2151409 1 8.11
CHEMBL2151413 1 8.11
CHEMBL2151414 1 7.66
CHEMBL2153751 1 7.64
CHEMBL2151407 1 7.32
CHEMBL2153752 1 6.85
CHEMBL2153756 1 6.52
CHEMBL2151406 1 -
CHEMBL2153754 1 -
CHEMBL2153753 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151411 IC50 = 0.2 nM 9.70
CHEMBL1996510 IC50 = 0.6 nM 9.22
CHEMBL2153750 IC50 = 1.2 nM 8.92
CHEMBL2151415 IC50 = 1.4 nM 8.85
CHEMBL568580 IC50 = 1.8 nM 8.74
CHEMBL565612 SOTRASTAURIN IC50 = 2.0 nM 8.70
CHEMBL2153748 IC50 = 2.0 nM 8.70
CHEMBL2153749 IC50 = 3.8 nM 8.42
CHEMBL2153755 IC50 = 5.0 nM 8.30
CHEMBL2151412 IC50 = 5.1 nM 8.29
CHEMBL2153747 IC50 = 5.2 nM 8.28
CHEMBL2151410 IC50 = 6.0 nM 8.22
CHEMBL2151408 IC50 = 6.5 nM 8.19
CHEMBL2151409 IC50 = 7.7 nM 8.11
CHEMBL2151413 IC50 = 7.8 nM 8.11
CHEMBL2151414 IC50 = 22.0 nM 7.66
CHEMBL2153751 IC50 = 23.0 nM 7.64
CHEMBL2151407 IC50 = 48.0 nM 7.32
CHEMBL2153752 IC50 = 140.0 nM 6.85
CHEMBL2153756 IC50 = 304.0 nM 6.52
CHEMBL2151406 IC50 > 316.0 nM -
CHEMBL2153754 IC50 > 316.0 nM -
CHEMBL2153753 IC50 > 316.0 nM -