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Compound Detail

CHEMBL224714

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CC(C)C[C@@H](NC(=O)OC(C)(C)C)C(=O)Nc1ccc(O)c2c(=O)cc(-c3ccccc3Cl)oc12

Basic Information

ChEMBL ID CHEMBL224714
Phase Preclinical
Structure Type MOL
InChI Key LVTCEBCCLKRNQN-GOSISDBHSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

501.0
MW (Da)
5.70
ALogP
6
HBA
3
HBD
117.9
PSA (Ų)
0.37
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29ClN2O6
MW 500.98
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.18

Activity Summary

IC50 3 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 5.6 5.6 2500.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.77 4.77 17000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 IC50 = 2500.0 nM 5.6 Antiproliferative activity against MCF7 cells 17123821
NON-PROTEIN TARGET IC50 = 17000.0 nM 4.77 Antiproliferative activity against ID8 cells 17123821

Literature References

PubMed DOI Target Context # Activities
17123821 10.1016/j.bmc.2006.10.063 NON-PROTEIN TARGET 1
17123821 10.1016/j.bmc.2006.10.063 MCF7 1
17123821 10.1016/j.bmc.2006.10.063 Cyclin-dependent kinase 2/cyclin A 1

Data from ChEMBL 36 via Core Engine