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Assay Detail

CHEMBL3268115

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

Binding
Displacement of [20-3H]PDBu from GST-tagged mouse PKC-delta C1B domain N7R mutant expressed in Escherichia coli after 2 to 30 mins by polyethylene glycol precipitation assay in presence of phosphatidylserine
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Diacylglycerol lactones targeting the structural features that distinguish the atypical C1 domains of protein kinase C ζ and ι from typical C1 domains.
Pu Y, Kang JH, Sigano DM, Peach ML, Lewin NE, Marquez VE, Blumberg PM.
J Med Chem (2014) 57 : 3835 -3844
PubMed 24684293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.48 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3262941 1 9.22
CHEMBL3262942 1 9.15
CHEMBL3262940 1 9.05
CHEMBL27768 1 8.93
CHEMBL380645 1 8.70
CHEMBL206889 1 8.61
CHEMBL209308 1 8.48
CHEMBL3262939 1 6.92
CHEMBL3262938 1 6.55
CHEMBL3262935 1 6.33
CHEMBL3262933 1 6.19
CHEMBL3262934 1 6.10
CHEMBL3262943 1 6.09
CHEMBL3262937 1 6.06
CHEMBL3262936 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3262941 Ki = 0.6 nM 9.22
CHEMBL3262942 Ki = 0.7 nM 9.15
CHEMBL3262940 Ki = 0.9 nM 9.05
CHEMBL27768 Ki = 1.18 nM 8.93
CHEMBL380645 Ki = 1.99 nM 8.70
CHEMBL206889 Ki = 2.48 nM 8.61
CHEMBL209308 Ki = 3.29 nM 8.48
CHEMBL3262939 Ki = 120.0 nM 6.92
CHEMBL3262938 Ki = 281.0 nM 6.55
CHEMBL3262935 Ki = 473.0 nM 6.33
CHEMBL3262933 Ki = 640.0 nM 6.19
CHEMBL3262934 Ki = 787.0 nM 6.10
CHEMBL3262943 Ki = 806.0 nM 6.09
CHEMBL3262937 Ki = 880.0 nM 6.06
CHEMBL3262936 Ki = 1737.0 nM 5.76