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Compound Detail

CHEMBL5596017

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COc1cc(Cc2c(-c3ccccc3)[nH]c3cc(C)ccc23)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL5596017
Phase Preclinical
Structure Type MOL
InChI Key PTIKSFBHIDVCFT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

387.5
MW (Da)
5.76
ALogP
3
HBA
1
HBD
43.5
PSA (Ų)
0.46
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25NO3
MW 387.48
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.10

Activity Summary

IC50 2 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
E3 ubiquitin-protein ligase Mdm2
CHEMBL5023
IC50 6.52 6.52 300.0 1
Protein Mdm4
CHEMBL1255126
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
E3 ubiquitin-protein ligase Mdm2 IC50 = 300.0 nM 6.52 Inhibition of MDM2 (unknown origin) 39185935
Protein Mdm4 IC50 = 100000.0 nM 4.0 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