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Compound Detail

CHEMBL4558879

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O=C1c2c(c3c4cccc(O)c4n([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)c3c3[nH]c4c(O)cccc4c23)C(=O)N1NC(CO)CO

Basic Information

ChEMBL ID CHEMBL4558879
Phase Preclinical
Structure Type MOL
InChI Key GCRUJJZDHHVZTG-FIVAAQFZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

608.6
MW (Da)
-0.73
ALogP
13
HBA
10
HBD
241.2
PSA (Ų)
0.11
QED
3
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28N4O11
MW 608.56
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness 0.94

Activity Summary

EC50 1 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
EC50 6.24 6.24 580.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 EC50 = 580.0 nM 6.24 Inhibition of topoisomerase-1 (unknown origin) using pBR 322 DNA as substrate 27687971

Literature References

PubMed DOI Target Context # Activities
27687971 10.1016/j.bmc.2016.09.045 DNA topoisomerase 1 1

Data from ChEMBL 36 via Core Engine