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Compound Detail

CHEMBL4518685

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COc1ccc(C[C@H](NC(=O)[C@H](C)NC(=O)CN2CCOCC2)C(=O)N[C@@H](C[C@@H]2CCCc3ccccc32)C(=O)[C@@]2(C)CO2)cc1

Basic Information

ChEMBL ID CHEMBL4518685
Phase Preclinical
Structure Type MOL
InChI Key KEJWJZGSUUQLSD-MSCSFMNWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

634.8
MW (Da)
1.91
ALogP
8
HBA
3
HBD
138.6
PSA (Ų)
0.27
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H46N4O7
MW 634.77
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness -0.32

Activity Summary

IC50 1 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome subunit beta type-10
CHEMBL3317334
IC50 5.6 5.6 2500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30657666 10.1021/acs.jmedchem.8b01884 Proteasome Macropain subunit 1
30657666 10.1021/acs.jmedchem.8b01884 Proteasome subunit beta type-10 1
30657666 10.1021/acs.jmedchem.8b01884 Proteasome Macropain subunit MB1 1
30657666 10.1021/acs.jmedchem.8b01884 Proteasome subunit beta type-8 1
30657666 10.1021/acs.jmedchem.8b01884 Proteasome component C5 1
30657666 10.1021/acs.jmedchem.8b01884 Proteasome subunit beta type-9 1

Data from ChEMBL 36 via Core Engine