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Compound Detail

CHEMBL102252

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CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(N)ccc3nc2-1

Basic Information

ChEMBL ID CHEMBL102252
Phase Preclinical
Structure Type MOL
InChI Key MVUUMBZAHAKPKQ-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
1.66
ALogP
7
HBA
2
HBD
107.4
PSA (Ų)
0.39
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17N3O4
MW 363.37
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness 0.97

Activity Summary

IC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 6.85 6.85 140.0 1

Pharmacokinetic Data

Parameter Value Units Species
KE 5.99 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase 1 IC50 = 140.0 nM 6.85 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 3
8410981 10.1021/jm00070a013 DNA topoisomerase 1 1
8410981 10.1021/jm00070a013 L1210 1
10447944 10.1021/jm9902279 Mus musculus 1
10447944 10.1021/jm9902279 Homo sapiens 1

Data from ChEMBL 36 via Core Engine