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Compound Detail

CHEMBL10741

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CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3c(C)cccc3nc2-1

Basic Information

ChEMBL ID CHEMBL10741
Phase Preclinical
Structure Type MOL
InChI Key OPQYKKOVPJTGSD-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

362.4
MW (Da)
2.39
ALogP
6
HBA
1
HBD
81.4
PSA (Ų)
0.53
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 C21H18N2O4
MW 362.39
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness 0.88

Activity Summary

IC50 2 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 1
CHEMBL1781
IC50 7.42 7.42 38.0 1
L1210
CHEMBL386
IC50 7.16 7.16 70.0 1

Pharmacokinetic Data

Parameter Value Units Species
KE 5.6 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8410981 10.1021/jm00070a013 Mus musculus 4
1846923 10.1021/jm00105a017 Mus musculus 2
1846923 10.1021/jm00105a017 DNA topoisomerase 1 1
1846923 10.1021/jm00105a017 L1210 1
8410981 10.1021/jm00070a013 DNA topoisomerase 1 1
8410981 10.1021/jm00070a013 L1210 1

Data from ChEMBL 36 via Core Engine