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Compound Detail

CHEMBL273734

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CCc1c2c(nc3cnc(Br)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC

Basic Information

ChEMBL ID CHEMBL273734
Phase Preclinical
Structure Type MOL
InChI Key GCCWSDCUPUCRPC-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

456.3
MW (Da)
2.80
ALogP
7
HBA
1
HBD
94.3
PSA (Ų)
0.37
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18BrN3O4
MW 456.30
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness 1.01

Activity Summary

IC50 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HT-29
CHEMBL384
IC50 8.15 8.15 7.0 1
DNA topoisomerase 1
CHEMBL1781
IC50 6.91 6.91 122.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7707314 10.1021/jm00007a008 HT-29 1
7707314 10.1021/jm00007a008 DNA topoisomerase 1 1

Data from ChEMBL 36 via Core Engine