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Assay Detail

CHEMBL871202

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

Binding
Displacement of [20-3H]PDBU from recombinant PKCalpha in presence of phosphatidylserine
35
Total Activities
35
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

Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.
Kang JH, Benzaria S, Sigano DM, Lewin NE, Pu Y, Peach ML, Blumberg PM, Marquez VE.
J Med Chem (2006) 49 : 3185 -3203
PubMed 16722637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.54 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210746 1 8.30
CHEMBL209666 1 8.15
CHEMBL208618 1 8.10
CHEMBL379945 1 8.05
CHEMBL110256 1 8.05
CHEMBL210666 1 8.05
CHEMBL380039 1 8.00
CHEMBL378783 1 7.92
CHEMBL377577 1 7.92
CHEMBL209779 1 7.85
CHEMBL209013 1 7.85
CHEMBL209140 1 7.85
CHEMBL379822 1 7.80
CHEMBL210495 1 7.80
CHEMBL209830 1 7.77
CHEMBL206889 1 7.77
CHEMBL377690 1 7.75
CHEMBL209938 1 7.75
CHEMBL380645 1 7.72
CHEMBL209308 1 7.66
CHEMBL206786 1 7.64
CHEMBL208417 1 7.62
CHEMBL210432 1 7.57
CHEMBL210725 1 7.55
CHEMBL210460 1 7.52
CHEMBL210196 1 7.44
CHEMBL208568 1 7.41
CHEMBL206735 1 7.36
CHEMBL109997 1 7.35
CHEMBL211049 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210746 Ki = 5.0 nM 8.30
CHEMBL209666 Ki = 7.0 nM 8.15
CHEMBL208618 Ki = 8.0 nM 8.10
CHEMBL379945 Ki = 9.0 nM 8.05
CHEMBL110256 Ki = 9.0 nM 8.05
CHEMBL210666 Ki = 9.0 nM 8.05
CHEMBL380039 Ki = 10.0 nM 8.00
CHEMBL378783 Ki = 12.0 nM 7.92
CHEMBL377577 Ki = 12.0 nM 7.92
CHEMBL209779 Ki = 14.0 nM 7.85
CHEMBL209013 Ki = 14.0 nM 7.85
CHEMBL209140 Ki = 14.0 nM 7.85
CHEMBL379822 Ki = 16.0 nM 7.80
CHEMBL210495 Ki = 16.0 nM 7.80
CHEMBL206889 Ki = 17.0 nM 7.77
CHEMBL209830 Ki = 17.0 nM 7.77
CHEMBL209938 Ki = 18.0 nM 7.75
CHEMBL377690 Ki = 18.0 nM 7.75
CHEMBL380645 Ki = 19.0 nM 7.72
CHEMBL209308 Ki = 22.0 nM 7.66
CHEMBL206786 Ki = 23.0 nM 7.64
CHEMBL208417 Ki = 24.0 nM 7.62
CHEMBL210432 Ki = 27.0 nM 7.57
CHEMBL210725 Ki = 28.0 nM 7.55
CHEMBL210460 Ki = 30.0 nM 7.52
CHEMBL210196 Ki = 36.0 nM 7.44
CHEMBL208568 Ki = 39.0 nM 7.41
CHEMBL206735 Ki = 44.0 nM 7.36
CHEMBL109997 Ki = 45.0 nM 7.35
CHEMBL211049 Ki = 67.0 nM 7.17
CHEMBL209184 Ki = 73.0 nM 7.14
CHEMBL209615 Ki = 406.0 nM 6.39
CHEMBL209616 Ki = 670.0 nM 6.17
CHEMBL209665 Ki = 983.0 nM 6.01
CHEMBL210547 Ki = 2400.0 nM 5.62