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Compound Detail

CHEMBL585540

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CCOC(=O)CNC(=O)/C=C\C(=O)N1C/C(=C\c2ccccc2)C(=O)/C(=C/c2ccccc2)C1

Basic Information

ChEMBL ID CHEMBL585540
Phase Preclinical
Structure Type MOL
InChI Key LOTBSJHRXJPYDK-FDGQHLOUSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

458.5
MW (Da)
2.80
ALogP
5
HBA
1
HBD
92.8
PSA (Ų)
0.51
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N2O5
MW 458.51
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.43

Activity Summary

IC50 3 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CCRF-CEM
CHEMBL382
IC50 5.89 5.89 1300.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.85 5.85 1400.0 1
L1210
CHEMBL386
IC50 5.21 5.21 6100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CCRF-CEM IC50 = 1300.0 nM 5.89 Cytotoxicity against human CEM cells 19819135
NON-PROTEIN TARGET IC50 = 1400.0 nM 5.85 Cytotoxicity against human Molt4/C8 cells 19819135
L1210 IC50 = 6100.0 nM 5.21 Cytotoxicity against mouse L1210 cells 19819135

Literature References

PubMed DOI Target Context # Activities
19819135 10.1016/j.bmcl.2009.09.069 DNA topoisomerase 2-alpha 4
19819135 10.1016/j.bmcl.2009.09.069 L1210 1
19819135 10.1016/j.bmcl.2009.09.069 NON-PROTEIN TARGET 1
19819135 10.1016/j.bmcl.2009.09.069 CCRF-CEM 1

Data from ChEMBL 36 via Core Engine