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Compound Detail

CHEMBL396036

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CCOC(=O)/C=C/[C@H](CCC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@H](CC(C)C)NC(=O)c1cccc(O)c1C

Basic Information

ChEMBL ID CHEMBL396036
Phase Preclinical
Structure Type MOL
InChI Key INLPEWSSLANRQY-NOMZNWIRSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

606.7
MW (Da)
2.67
ALogP
7
HBA
4
HBD
168.1
PSA (Ų)
0.20
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 C33H42N4O7
MW 606.72
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -0.09

Activity Summary

IC50 1 meas. best 5.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.23 5.23 5890.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 6.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 5890.0 nM 5.23 Inhibition of trypsin-like activity of 20S proteasome in lymphoblastoid cells af... 17291631

Literature References

PubMed DOI Target Context # Activities
17291631 10.1016/j.ejmech.2006.12.008 Unchecked 3
17291631 10.1016/j.ejmech.2006.12.008 Plasma 1

Data from ChEMBL 36 via Core Engine