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Compound Detail

CHEMBL337535

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COC1C(CO)OC(n2c3ccccc3c3c4c(c5c6ccccc6[nH]c5c32)CNC4=O)C(O)C1O

Basic Information

ChEMBL ID CHEMBL337535
Phase Preclinical
Structure Type MOL
InChI Key RCARSYAJRLTMFI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

487.5
MW (Da)
2.30
ALogP
7
HBA
5
HBD
129.0
PSA (Ų)
0.27
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N3O6
MW 487.51
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness 1.24

Activity Summary

IC50 2 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P388
CHEMBL389
IC50 5.52 5.52 3000.0 1
Protein kinase C alpha type
CHEMBL299
IC50 5.43 5.43 3700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P388 IC50 = 3000.0 nM 5.52 Antiproliferative activity against P388 Murine Leukemia cells 8893841
Protein kinase C alpha type IC50 = 3700.0 nM 5.43 Inhibition of Protein Kinase C(PKC) 8893841

Literature References

PubMed DOI Target Context # Activities
8893841 10.1021/jm9603779 Protein kinase C alpha type 1
8893841 10.1021/jm9603779 Unchecked 1
8893841 10.1021/jm9603779 B16 1
8893841 10.1021/jm9603779 P388 1
8893841 10.1021/jm9603779 DNA topoisomerase 1 1
8893841 10.1021/jm9603779 DNA topoisomerase 2-beta 1
8893841 10.1021/jm9603779 Bacillus cereus 1

Data from ChEMBL 36 via Core Engine