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Compound Detail

CHEMBL188781

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CCOC(=O)/C=C/[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)OCc1ccccc1)C(C)C

Basic Information

ChEMBL ID CHEMBL188781
Phase Preclinical
Structure Type MOL
InChI Key XVQOTACKHQVYOY-FHTSGJMESA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

505.6
MW (Da)
2.06
ALogP
7
HBA
4
HBD
143.1
PSA (Ų)
0.22
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H39N3O7
MW 505.61
Aromatic Rings 1
Heavy Atoms 36
NP-Likeness 0.22

Activity Summary

IC50 1 meas. best 7.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome
CHEMBL612443
IC50 7.15 7.15 71.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 3.967 hr Homo sapiens
T1/2 6.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteasome IC50 = 71.0 nM 7.15 Inhibition of trypsin like activity of the proteasome purified from lymphoblasto... 16033282

Literature References

PubMed DOI Target Context # Activities
16033282 10.1021/jm040905d Proteasome 3
16033282 10.1021/jm040905d ADMET 2

Data from ChEMBL 36 via Core Engine