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Assay Detail

CHEMBL769346

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Binding
Inhibition of Protein Kinase C(PKC)
23
Total Activities
23
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

Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.
Pereira ER, Belin L, Sancelme M, Prudhomme M, Ollier M, Rapp M, Sevère D, Riou JF, Fabbro D, Meyer T.
J Med Chem (1996) 39 : 4471 -4477
PubMed 8893841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 4.57 5.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16958 STAUROSPORINONE 1 5.61
CHEMBL337535 1 5.43
CHEMBL127277 1 4.66
CHEMBL343788 1 4.54
CHEMBL335373 1 4.40
CHEMBL138041 1 4.36
CHEMBL268368 STAUROSPORINE AGLYCON 1 4.35
CHEMBL138039 1 4.17
CHEMBL142141 1 4.11
CHEMBL140891 1 4.10
CHEMBL343990 1 -
CHEMBL139517 1 -
CHEMBL137842 1 -
CHEMBL138757 1 -
CHEMBL422107 1 -
CHEMBL335122 1 -
CHEMBL137907 1 -
CHEMBL3350557 1 -
CHEMBL370100 REBECCAMYCIN 1 -
CHEMBL138203 1 -
CHEMBL435422 1 -
CHEMBL335822 1 -
CHEMBL139266 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16958 STAUROSPORINONE IC50 = 2450.0 nM 5.61
CHEMBL337535 IC50 = 3700.0 nM 5.43
CHEMBL127277 IC50 = 22100.0 nM 4.66
CHEMBL343788 IC50 = 28800.0 nM 4.54
CHEMBL335373 IC50 = 40000.0 nM 4.40
CHEMBL138041 IC50 = 43500.0 nM 4.36
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 44700.0 nM 4.35
CHEMBL138039 IC50 = 68000.0 nM 4.17
CHEMBL142141 IC50 = 78000.0 nM 4.11
CHEMBL140891 IC50 = 79200.0 nM 4.10
CHEMBL343990 IC50 > 100000.0 nM -
CHEMBL139517 IC50 > 100000.0 nM -
CHEMBL137842 IC50 > 100000.0 nM -
CHEMBL138757 IC50 > 100000.0 nM -
CHEMBL422107 IC50 > 100000.0 nM -
CHEMBL335122 IC50 > 100000.0 nM -
CHEMBL137907 IC50 > 100000.0 nM -
CHEMBL3350557 IC50 > 100000.0 nM -
CHEMBL370100 REBECCAMYCIN IC50 > 100000.0 nM -
CHEMBL138203 IC50 > 100000.0 nM -
CHEMBL435422 IC50 > 100000.0 nM -
CHEMBL335822 IC50 > 100000.0 nM -
CHEMBL139266 IC50 > 100000.0 nM -