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Compound Detail

CHEMBL2114241

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CC[C@@](O)(C(=O)[O-])c1cc2n(c(=O)c1CO)Cc1cc3cc4c(cc3nc1-2)OCO4.[Na+]

Basic Information

ChEMBL ID CHEMBL2114241
Phase Preclinical
Structure Type MOL
InChI Key WQMQVBDSWGBSTI-BOXHHOBZSA-M
Parent Compound CHEMBL2219791
Active Moiety CHEMBL2219791
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

410.4
MW (Da)
1.33
ALogP
8
HBA
3
HBD
131.1
PSA (Ų)
0.46
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17N2NaO7
MW 432.36
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness 0.51

Activity Summary

IC50 1 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 6.08 6.08 840.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 IC50 = 840.0 nM 6.08 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 Mus musculus 2
8410981 10.1021/jm00070a013 DNA topoisomerase 1 1
8410981 10.1021/jm00070a013 Unchecked 1
8410981 10.1021/jm00070a013 HT-29 1

Data from ChEMBL 36 via Core Engine