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Assay Detail

CHEMBL769111

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Binding
Evaluated against recombinant human Protein kinase C epsilon
26
Total Activities
25
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 epsilon type (CHEMBL3582)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Defauw JM, Murphy MM, Jagdmann GE, Hu H, Lampe JW, Hollinshead SP, Mitchell TJ, Crane HM, Heerding JM, Mendoza JS, Davis JE, Darges JW, Hubbard FR, Hall SE.
J Med Chem (1996) 39 : 5215 -5227
PubMed 8978850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.82 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300422 1 7.70
CHEMBL60254 BALANOL 1 7.70
CHEMBL49354 1 7.42
CHEMBL48636 1 7.30
CHEMBL295806 2 6.92
CHEMBL48988 1 6.62
CHEMBL148745 1 6.55
CHEMBL358264 1 6.50
CHEMBL345767 1 6.34
CHEMBL151822 1 5.64
CHEMBL48546 1 5.40
CHEMBL151800 1 5.39
CHEMBL48665 1 5.35
CHEMBL149313 1 4.89
CHEMBL149873 1 4.89
CHEMBL146846 1 4.82
CHEMBL439996 1 4.52
CHEMBL421790 1 4.52
CHEMBL146847 1 4.42
CHEMBL151823 1 4.41
CHEMBL150264 1 4.33
CHEMBL150422 1 -
CHEMBL151731 1 -
CHEMBL343362 1 -
CHEMBL149604 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300422 IC50 = 20.0 nM 7.70
CHEMBL60254 BALANOL IC50 = 20.0 nM 7.70
CHEMBL49354 IC50 = 38.0 nM 7.42
CHEMBL48636 IC50 = 50.0 nM 7.30
CHEMBL295806 IC50 = 120.0 nM 6.92
CHEMBL48988 IC50 = 240.0 nM 6.62
CHEMBL148745 IC50 = 280.0 nM 6.55
CHEMBL358264 IC50 = 320.0 nM 6.50
CHEMBL345767 IC50 = 460.0 nM 6.34
CHEMBL295806 IC50 = 500.0 nM 6.30
CHEMBL151822 IC50 = 2300.0 nM 5.64
CHEMBL48546 IC50 = 4000.0 nM 5.40
CHEMBL151800 IC50 = 4100.0 nM 5.39
CHEMBL48665 IC50 = 4500.0 nM 5.35
CHEMBL149873 IC50 = 13000.0 nM 4.89
CHEMBL149313 IC50 = 13000.0 nM 4.89
CHEMBL146846 IC50 = 15000.0 nM 4.82
CHEMBL439996 IC50 = 30000.0 nM 4.52
CHEMBL421790 IC50 = 30000.0 nM 4.52
CHEMBL146847 IC50 = 38000.0 nM 4.42
CHEMBL151823 IC50 = 39000.0 nM 4.41
CHEMBL150264 IC50 = 47000.0 nM 4.33
CHEMBL150422 IC50 > 50000.0 nM -
CHEMBL151731 IC50 > 50000.0 nM -
CHEMBL343362 IC50 > 50000.0 nM -
CHEMBL149604 IC50 > 50000.0 nM -