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Assay Detail

CHEMBL2330915

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

Binding
Inhibition of PKC delta (unknown origin) using ERMRPRKRQGSVRRRV as substrate after 15 mins by spectrophotometry in presence of ATP
27
Total Activities
27
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 delta type (CHEMBL2996)
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
Ki 27 6.75 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326002 1 7.80
CHEMBL2326001 1 7.75
CHEMBL2326007 1 7.24
CHEMBL2046626 1 7.10
CHEMBL2326016 1 7.09
CHEMBL2326019 1 7.05
CHEMBL2326009 1 6.92
CHEMBL2326004 1 6.89
CHEMBL2326017 1 6.88
CHEMBL2326018 1 6.88
CHEMBL2326020 1 6.82
CHEMBL2325999 1 6.62
CHEMBL2046624 1 6.59
CHEMBL2321918 1 6.47
CHEMBL2326003 1 6.45
CHEMBL2326011 1 6.32
CHEMBL2326014 1 6.28
CHEMBL2326012 1 6.26
CHEMBL2326015 1 6.14
CHEMBL2326021 1 6.10
CHEMBL2326013 1 6.02
CHEMBL2326005 1 -
CHEMBL2326006 1 -
CHEMBL2326008 1 -
CHEMBL2326010 1 -
CHEMBL2325998 1 -
CHEMBL2326000 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326002 Ki = 16.0 nM 7.80
CHEMBL2326001 Ki = 18.0 nM 7.75
CHEMBL2326007 Ki = 57.0 nM 7.24
CHEMBL2046626 Ki = 80.0 nM 7.10
CHEMBL2326016 Ki = 81.0 nM 7.09
CHEMBL2326019 Ki = 89.0 nM 7.05
CHEMBL2326009 Ki = 120.0 nM 6.92
CHEMBL2326004 Ki = 130.0 nM 6.89
CHEMBL2326017 Ki = 132.0 nM 6.88
CHEMBL2326018 Ki = 131.0 nM 6.88
CHEMBL2326020 Ki = 151.0 nM 6.82
CHEMBL2325999 Ki = 242.0 nM 6.62
CHEMBL2046624 Ki = 255.0 nM 6.59
CHEMBL2321918 Ki = 336.0 nM 6.47
CHEMBL2326003 Ki = 358.0 nM 6.45
CHEMBL2326011 Ki = 480.0 nM 6.32
CHEMBL2326014 Ki = 526.0 nM 6.28
CHEMBL2326012 Ki = 547.0 nM 6.26
CHEMBL2326015 Ki = 722.0 nM 6.14
CHEMBL2326021 Ki = 792.0 nM 6.10
CHEMBL2326013 Ki = 957.0 nM 6.02
CHEMBL2326005 Ki > 1250.0 nM -
CHEMBL2326006 Ki > 1250.0 nM -
CHEMBL2326008 Ki > 1250.0 nM -
CHEMBL2326010 Ki > 1250.0 nM -
CHEMBL2325998 Ki < 10.0 nM -
CHEMBL2326000 Ki < 10.0 nM -