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Compound Detail

CHEMBL5081898

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COc1ccc(NC(=O)c2cccnc2Nc2cccc(Cl)c2C)cc1

Basic Information

ChEMBL ID CHEMBL5081898
Phase Preclinical
Structure Type MOL
InChI Key LMRZMKVQRBRGBG-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

367.8
MW (Da)
5.05
ALogP
4
HBA
2
HBD
63.2
PSA (Ų)
0.66
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H18ClN3O2
MW 367.84
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.76

Activity Summary

IC50 2 meas. best 4.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 4.21 4.21 61200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 IC50 = 61200.0 nM 4.21 Inhibition of human topoisomerase I using DNA pBR322 as substrate assessed as DN... 34537445

Literature References

PubMed DOI Target Context # Activities
34537445 10.1016/j.ejmech.2021.113817 U-87 MG 1
34537445 10.1016/j.ejmech.2021.113817 U-251 1
34537445 10.1016/j.ejmech.2021.113817 C6 1
34537445 10.1016/j.ejmech.2021.113817 Prostaglandin G/H synthase 2 1
34537445 10.1016/j.ejmech.2021.113817 DNA topoisomerase 1 1

Data from ChEMBL 36 via Core Engine