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Assay Detail

CHEMBL860607

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

Binding
Displacement of [20-3H]PDBu from recombinant PKC alpha in presence of phosphatidylserine
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein kinase C alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators.
Lee J, Kang JH, Han KC, Kim Y, Kim SY, Youn HS, Mook-Jung I, Kim H, Lo Han JH, Ha HJ, Kim YH, Marquez VE, Lewin NE, Pearce LV, Lundberg DJ, Blumberg PM.
J Med Chem (2006) 49 : 2028 -2036
PubMed 16539391 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.51 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203524 1 8.84
CHEMBL96766 1 8.54
CHEMBL383615 1 8.42
CHEMBL137386 1 8.35
CHEMBL138171 1 8.35
CHEMBL206332 1 8.30
CHEMBL383708 1 8.22
CHEMBL203521 1 8.21
CHEMBL382784 1 8.18
CHEMBL137597 1 8.16
CHEMBL203607 1 8.16
CHEMBL380661 1 7.79
CHEMBL204134 1 7.75
CHEMBL206605 1 7.55
CHEMBL205619 1 7.32
CHEMBL205248 1 6.89
CHEMBL205670 1 6.83
CHEMBL381693 1 6.76
CHEMBL206485 1 5.68
CHEMBL378380 1 4.74
CHEMBL436943 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203524 Ki = 1.45 nM 8.84
CHEMBL96766 Ki = 2.9 nM 8.54
CHEMBL383615 Ki = 3.78 nM 8.42
CHEMBL137386 Ki = 4.51 nM 8.35
CHEMBL138171 Ki = 4.46 nM 8.35
CHEMBL206332 Ki = 4.97 nM 8.30
CHEMBL383708 Ki = 6.04 nM 8.22
CHEMBL203521 Ki = 6.18 nM 8.21
CHEMBL382784 Ki = 6.66 nM 8.18
CHEMBL137597 Ki = 6.87 nM 8.16
CHEMBL203607 Ki = 6.88 nM 8.16
CHEMBL380661 Ki = 16.1 nM 7.79
CHEMBL204134 Ki = 18.0 nM 7.75
CHEMBL206605 Ki = 28.0 nM 7.55
CHEMBL205619 Ki = 48.0 nM 7.32
CHEMBL205248 Ki = 129.0 nM 6.89
CHEMBL205670 Ki = 147.0 nM 6.83
CHEMBL381693 Ki = 173.0 nM 6.76
CHEMBL206485 Ki = 2100.0 nM 5.68
CHEMBL378380 Ki = 18300.0 nM 4.74
CHEMBL436943 Ki = 21700.0 nM 4.66