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Compound Detail

CHEMBL2115022

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CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc([N+](=O)[O-])ccc3nc2-1

Basic Information

ChEMBL ID CHEMBL2115022
Phase Preclinical
Structure Type MOL
InChI Key XLHNAFUKOSPOAT-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

393.4
MW (Da)
1.99
ALogP
8
HBA
1
HBD
124.6
PSA (Ų)
0.31
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15N3O6
MW 393.36
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness 0.48

Activity Summary

IC50 1 meas. best 6.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 6.19 6.19 640.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 IC50 = 640.0 nM 6.19 Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells 8410981

Literature References

PubMed DOI Target Context # Activities
8410981 10.1021/jm00070a013 DNA topoisomerase 1 1

Data from ChEMBL 36 via Core Engine