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Compound Detail

CHEMBL5591432

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O=C(Nc1cccc(-n2ccc(-c3ccccc3)n2)c1)C1=NN(c2ccc(Cl)cc2)[C@]2(C(=O)Nc3cc(Cl)ccc32)[C@H]1c1cccc(O)c1

Basic Information

ChEMBL ID CHEMBL5591432
Phase Preclinical
Structure Type MOL
InChI Key MMVJKWGROZJXQD-UVNLRBHVSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

685.6
MW (Da)
8.00
ALogP
7
HBA
3
HBD
111.8
PSA (Ų)
0.16
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H26Cl2N6O3
MW 685.57
Aromatic Rings 6
Heavy Atoms 49
NP-Likeness -0.89

Activity Summary

IC50 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
E3 ubiquitin-protein ligase Mdm2
CHEMBL5023
IC50 7.52 7.52 30.0 1
Protein Mdm4
CHEMBL1255126
IC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
E3 ubiquitin-protein ligase Mdm2 IC50 = 30.0 nM 7.52 Inhibition of MDM2 (unknown origin) 39185935
Protein Mdm4 IC50 = 200.0 nM 6.7 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