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Compound Detail

CHEMBL5592473

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CCOC(=O)C1=NN(c2ccc(Cl)cc2)[C@]2(C(=O)Nc3cc(Cl)ccc32)[C@H]1c1cccc(Cl)c1F

Basic Information

ChEMBL ID CHEMBL5592473
Phase Preclinical
Structure Type MOL
InChI Key HIUSVJZXJUTUQG-CPJSRVTESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

532.8
MW (Da)
6.16
ALogP
5
HBA
1
HBD
71.0
PSA (Ų)
0.41
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H17Cl3FN3O3
MW 532.79
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.71

Activity Summary

IC50 2 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
E3 ubiquitin-protein ligase Mdm2
CHEMBL5023
IC50 7.16 7.16 70.0 1
Protein Mdm4
CHEMBL1255126
IC50 7.1 7.1 80.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
E3 ubiquitin-protein ligase Mdm2 IC50 = 70.0 nM 7.16 Inhibition of MDM2 (unknown origin) 39185935
Protein Mdm4 IC50 = 80.0 nM 7.1 Inhibition of MDMX (unknown origin) 39185935

Literature References

PubMed DOI Target Context # Activities
39185935 10.1021/acs.jmedchem.4c00913 Protein Mdm4 1
39185935 10.1021/acs.jmedchem.4c00913 E3 ubiquitin-protein ligase Mdm2 1

Data from ChEMBL 36 via Core Engine