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Assay Detail

CHEMBL769620

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Binding
Affinity for protein kinase-C alpha (PK-C alpha)
14
Total Activities
14
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 (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.
Tamamura H, Bienfait B, Nacro K, Lewin NE, Blumberg PM, Marquez VE.
J Med Chem (2000) 43 : 3210 -3217
PubMed 10966739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.77 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111625 1 8.64
CHEMBL290876 1 8.54
CHEMBL107614 1 7.89
CHEMBL321823 1 7.62
CHEMBL94492 1 7.02
CHEMBL107602 1 6.49
CHEMBL109099 1 6.30
CHEMBL420668 1 6.25
CHEMBL320984 1 6.24
CHEMBL320520 1 6.17
CHEMBL108443 1 6.00
CHEMBL108397 1 5.96
CHEMBL108303 1 5.92
CHEMBL109630 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111625 Ki = 2.3 nM 8.64
CHEMBL290876 Ki = 2.9 nM 8.54
CHEMBL107614 Ki = 13.0 nM 7.89
CHEMBL321823 Ki = 24.0 nM 7.62
CHEMBL94492 Ki = 96.0 nM 7.02
CHEMBL107602 Ki = 327.0 nM 6.49
CHEMBL109099 Ki = 499.0 nM 6.30
CHEMBL420668 Ki = 565.0 nM 6.25
CHEMBL320984 Ki = 579.0 nM 6.24
CHEMBL320520 Ki = 679.0 nM 6.17
CHEMBL108443 Ki = 1000.0 nM 6.00
CHEMBL108397 Ki = 1088.0 nM 5.96
CHEMBL108303 Ki = 1202.0 nM 5.92
CHEMBL109630 Ki = 1758.0 nM 5.75