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Compound Detail

CHEMBL130381

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Cc1cc(-c2c(F)cc3c4nn(CCN(C)C)c(=O)c-4cn(C4CC4)c3c2F)cc(C)n1

Basic Information

ChEMBL ID CHEMBL130381
Phase Preclinical
Structure Type MOL
InChI Key PGJDQMYHNOXAEZ-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

437.5
MW (Da)
4.16
ALogP
6
HBA
0
HBD
56.0
PSA (Ų)
0.47
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25F2N5O
MW 437.49
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.13

Activity Summary

EC50 2 meas. best 6.03
IC50 1 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P388
CHEMBL389
IC50 6.58 6.58 260.0 1
DNA topoisomerase 2-beta
CHEMBL3396
EC50 6.03 6.03 930.0 1
DNA topoisomerase II
CHEMBL2094255
EC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00044-T Mus musculus 2
- 10.1016/0960-894X(95)00044-T DNA topoisomerase II 1
- 10.1016/0960-894X(95)00044-T P388 1
- 10.1016/0960-894X(95)00044-T DNA topoisomerase 2-beta 1

Data from ChEMBL 36 via Core Engine