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Compound Detail

CHEMBL418951

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CCC(O)(C(=O)[O-])c1cc2n(c(=O)c1CO)Cc1cc3cc([O-])ccc3nc1-2.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL418951
Phase Preclinical
Structure Type MOL
InChI Key YDXUCVGOGIDHLM-UHFFFAOYSA-L
Parent Compound CHEMBL1207601
Active Moiety CHEMBL1207601
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

382.4
MW (Da)
1.31
ALogP
7
HBA
4
HBD
132.9
PSA (Ų)
0.42
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 C20H16N2Na2O6
MW 426.34
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness 0.73

Activity Summary

IC50 1 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 5.5 5.5 3200.0 1

Pharmacokinetic Data

Parameter Value Units Species
KE 3.24 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 IC50 = 3200.0 nM 5.5 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 4
8410981 10.1021/jm00070a013 DNA topoisomerase 1 1
8410981 10.1021/jm00070a013 L1210 1

Data from ChEMBL 36 via Core Engine