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Compound Detail

CHEMBL540569

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CCC1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3c(NC(=O)CN)c4c(cc3nc2-1)OCO4.Cl

Basic Information

ChEMBL ID CHEMBL540569
Phase Preclinical
Structure Type MOL
InChI Key LGULSCBEVPJHFZ-UHFFFAOYSA-N
Parent Compound CHEMBL1190295
Active Moiety CHEMBL1190295
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

464.4
MW (Da)
0.71
ALogP
10
HBA
3
HBD
155.0
PSA (Ų)
0.37
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 C23H21ClN4O7
MW 500.90
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness 0.75

Activity Summary

IC50 1 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 6.58 6.58 260.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 IC50 = 260.0 nM 6.58 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 2

Data from ChEMBL 36 via Core Engine