Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4004544

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

Binding
Inhibition of PKCtheta (unknown origin) after 60 mins in presence of [gamma33P]ATP by scintillation proximity assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein kinase C theta type (CHEMBL3920)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β.
van Eis MJ, Evenou J, Schuler W, Zenke G, Vangrevelinghe E, Wagner J, von Matt P.
Bioorg Med Chem Lett (2017) 27 : 781 -786
PubMed 28131714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.26 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565612 SOTRASTAURIN 2.0 1 9.00
CHEMBL4085837 1 7.92
CHEMBL4064291 1 7.72
CHEMBL4072879 1 7.68
CHEMBL4101316 1 7.68
CHEMBL4083319 1 7.00
CHEMBL4102228 1 6.67
CHEMBL4089217 1 6.59
CHEMBL4077967 1 6.58
CHEMBL4072709 1 6.56
CHEMBL4068028 1 6.50
CHEMBL4073977 1 -
CHEMBL4083182 1 -
CHEMBL4100747 1 -
CHEMBL4089665 1 -
CHEMBL4078759 1 -
CHEMBL4099609 1 -
CHEMBL4061321 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565612 SOTRASTAURIN IC50 = 1.0 nM 9.00
CHEMBL4085837 IC50 = 12.0 nM 7.92
CHEMBL4064291 IC50 = 19.0 nM 7.72
CHEMBL4072879 IC50 = 21.0 nM 7.68
CHEMBL4101316 IC50 = 21.0 nM 7.68
CHEMBL4083319 IC50 = 101.0 nM 7.00
CHEMBL4102228 IC50 = 216.0 nM 6.67
CHEMBL4089217 IC50 = 254.0 nM 6.59
CHEMBL4077967 IC50 = 263.0 nM 6.58
CHEMBL4072709 IC50 = 276.0 nM 6.56
CHEMBL4068028 IC50 = 314.0 nM 6.50
CHEMBL4073977 IC50 > 316.0 nM -
CHEMBL4083182 IC50 > 316.0 nM -
CHEMBL4100747 IC50 > 316.0 nM -
CHEMBL4089665 IC50 > 316.0 nM -
CHEMBL4078759 IC50 > 316.0 nM -
CHEMBL4099609 IC50 > 316.0 nM -
CHEMBL4061321 IC50 > 316.0 nM -