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Compound Detail

CHEMBL398742

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NCCCC[C@@H]1NC(=O)c2coc(n2)-c2coc(n2)-c2coc(n2)[C@H](CCCCN)NC(=O)c2coc(n2)-c2coc(n2)-c2coc1n2

Basic Information

ChEMBL ID CHEMBL398742
Phase Preclinical
Structure Type MOL
InChI Key DUCRIXKXJZZDHT-HOTGVXAUSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

658.6
MW (Da)
3.80
ALogP
16
HBA
4
HBD
266.4
PSA (Ų)
0.17
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H30N10O8
MW 658.63
Aromatic Rings 6
Heavy Atoms 48
NP-Likeness 0.28

Activity Summary

IC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Telomerase reverse transcriptase
CHEMBL2916
IC50 7.7 7.7 20.0 1
HeLa
CHEMBL399
IC50 5.13 5.13 7400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Telomerase reverse transcriptase IC50 = 20.0 nM 7.7 Inhibition of telomerase (unknown origin) by TRAP assay -
HeLa IC50 = 7400.0 nM 5.13 Cytotoxicity against human HeLa cells -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C2MD20234D Unchecked 13
20409709 10.1016/j.bmcl.2010.03.086 NON-PROTEIN TARGET 4
18248989 10.1016/j.bmcl.2007.12.048 Unchecked 2
- 10.1039/C0MD00241K Telomerase reverse transcriptase 1
- 10.1039/C0MD00241K HeLa 1

Data from ChEMBL 36 via Core Engine