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Assay Detail

CHEMBL2330912

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

Binding
Inhibition of PKC-theta in human PBMC cells assessed as inhibition of IL-2 after 24 hrs by bead-based FLISA assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases.
Jimenez JM, Boyall D, Brenchley G, Collier PN, Davis CJ, Fraysse D, Keily SB, Henderson J, Miller A, Pierard F, Settimo L, Twin HC, Bolton CM, Curnock AP, Chiu P, Tanner AJ, Young S.
J Med Chem (2013) 56 : 1799 -1810
PubMed 23398373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.79 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326000 1 9.00
CHEMBL2326001 1 8.70
CHEMBL2325998 1 8.40
CHEMBL2326007 1 8.22
CHEMBL2326002 1 7.96
CHEMBL2325999 1 6.92
CHEMBL2326012 1 6.77
CHEMBL2326013 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326000 IC50 = 1.0 nM 9.00
CHEMBL2326001 IC50 = 2.0 nM 8.70
CHEMBL2325998 IC50 = 4.0 nM 8.40
CHEMBL2326007 IC50 = 6.0 nM 8.22
CHEMBL2326002 IC50 = 11.0 nM 7.96
CHEMBL2325999 IC50 = 120.0 nM 6.92
CHEMBL2326012 IC50 = 170.0 nM 6.77
CHEMBL2326013 IC50 = 420.0 nM 6.38