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Assay Detail

CHEMBL767471

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

Binding
Inhibitory concentration required against Protein kinase C (isolated from rat brain) in PKC assay performed with 4 ug phosphatidyl serine:diacylglycerol (2:1)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Protein kinase C (PKC) (CHEMBL2094266)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Aryl-fused sphingolipids as novel PKC inhibitors with topical antiinflammatory activity
Tegeler JJ, Rauckman BS, Hamer RL, Freed BS, Merriman GH, Hellyer L, Ortega-Nanos M, Bailey SC, Kurtz ES
Bioorg Med Chem Lett (1995) 5 : 2477 -2482
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.03 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84654 1 5.57
CHEMBL82271 1 5.54
CHEMBL82095 1 5.46
CHEMBL83961 1 5.43
CHEMBL79293 1 5.35
CHEMBL309649 1 5.33
CHEMBL86221 1 5.30
CHEMBL67166 SPHINGOSINE 1 5.17
CHEMBL86219 1 5.04
CHEMBL450573 1 5.01
CHEMBL83595 1 5.00
CHEMBL315198 1 5.00
CHEMBL83281 1 5.00
CHEMBL312617 1 4.97
CHEMBL80054 1 4.96
CHEMBL83733 1 4.88
CHEMBL79775 1 4.85
CHEMBL315574 1 4.80
CHEMBL79330 1 4.70
CHEMBL79284 1 4.52
CHEMBL311408 1 4.44
CHEMBL310407 1 4.36
CHEMBL81533 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84654 IC50 = 2700.0 nM 5.57
CHEMBL82271 IC50 = 2900.0 nM 5.54
CHEMBL82095 IC50 = 3500.0 nM 5.46
CHEMBL83961 IC50 = 3700.0 nM 5.43
CHEMBL79293 IC50 = 4500.0 nM 5.35
CHEMBL309649 IC50 = 4700.0 nM 5.33
CHEMBL86221 IC50 = 5000.0 nM 5.30
CHEMBL67166 SPHINGOSINE IC50 = 6700.0 nM 5.17
CHEMBL86219 IC50 = 9100.0 nM 5.04
CHEMBL450573 IC50 = 9700.0 nM 5.01
CHEMBL83595 IC50 = 10000.0 nM 5.00
CHEMBL315198 IC50 = 10000.0 nM 5.00
CHEMBL83281 IC50 = 10000.0 nM 5.00
CHEMBL312617 IC50 = 10800.0 nM 4.97
CHEMBL80054 IC50 = 10900.0 nM 4.96
CHEMBL83733 IC50 = 13300.0 nM 4.88
CHEMBL79775 IC50 = 14000.0 nM 4.85
CHEMBL315574 IC50 = 15900.0 nM 4.80
CHEMBL79330 IC50 = 19900.0 nM 4.70
CHEMBL79284 IC50 = 30500.0 nM 4.52
CHEMBL311408 IC50 = 36000.0 nM 4.44
CHEMBL310407 IC50 = 43900.0 nM 4.36
CHEMBL81533 IC50 > 100000.0 nM -