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Assay Detail

CHEMBL760366

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

Binding
Displacement of [20-3H]-PDBU ligand from recombinant protein kinase C (baculovirus)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous 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. 18. The incorporation of a hydroxamate moiety into diacylglycerol-lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase C (PK-C). Implications for isozyme specificity.
Lee J, Han KC, Kang JH, Pearce LL, Lewin NE, Yan S, Benzaria S, Nicklaus MC, Blumberg PM, Marquez VE.
J Med Chem (2001) 44 : 4309 -4312
PubMed 11728178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.40 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137288 1 8.57
CHEMBL290876 1 8.54
CHEMBL96766 1 8.54
CHEMBL138171 1 8.35
CHEMBL137386 1 8.35
CHEMBL135779 1 8.32
CHEMBL94505 1 8.27
CHEMBL137597 1 8.16
CHEMBL137701 1 8.08
CHEMBL136760 1 7.95
CHEMBL136786 1 6.37
CHEMBL439979 1 5.90
CHEMBL336926 1 5.36
CHEMBL137484 1 5.32
CHEMBL138279 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137288 Ki = 2.7 nM 8.57
CHEMBL290876 Ki = 2.89 nM 8.54
CHEMBL96766 Ki = 2.9 nM 8.54
CHEMBL138171 Ki = 4.46 nM 8.35
CHEMBL137386 Ki = 4.51 nM 8.35
CHEMBL135779 Ki = 4.81 nM 8.32
CHEMBL94505 Ki = 5.42 nM 8.27
CHEMBL137597 Ki = 6.87 nM 8.16
CHEMBL137701 Ki = 8.32 nM 8.08
CHEMBL136760 Ki = 11.25 nM 7.95
CHEMBL136786 Ki = 429.7 nM 6.37
CHEMBL439979 Ki = 1260.0 nM 5.90
CHEMBL336926 Ki = 4330.0 nM 5.36
CHEMBL137484 Ki = 4840.0 nM 5.32
CHEMBL138279 Ki = 10430.0 nM 4.98