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Compound Detail

CHEMBL3218828

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Cc1cc(C(=O)N[C@@H](CC(=O)NCC(C)(C)C)C(=O)N[C@@H](CCc2ccccc2)C(=O)NCc2ccccc2)no1

Basic Information

ChEMBL ID CHEMBL3218828
Phase Preclinical
Structure Type MOL
InChI Key PEKNSUNAKRRBMR-DQEYMECFSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
3.07
ALogP
6
HBA
4
HBD
142.4
PSA (Ų)
0.25
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H39N5O5
MW 561.68
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.93

Activity Summary

IC50 3 meas. best 8.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome Macropain subunit MB1
CHEMBL4662
IC50 8.33 7.965 4.7 2
Nuclear factor NF-kappa-B complex
CHEMBL2094258
IC50 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C2MD20060K Proteasome Macropain subunit MB1 2
- 10.1039/C2MD20060K Proteasome component C5 1
- 10.1039/C2MD20060K Proteasome Macropain subunit 1
- 10.1039/C2MD20060K Nuclear factor NF-kappa-B complex 1
- 10.1039/C2MD20060K NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine