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Compound Detail

CHEMBL207598

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COC[C@H](NC(=O)[C@H](CC(=O)NCC(C)(C)C)NS(=O)(=O)c1ccc(C)cc1)C(=O)N[C@@H](CC(C)C)C(=O)c1nnc(-c2ccc(N(C)C)cc2)o1

Basic Information

ChEMBL ID CHEMBL207598
Phase Preclinical
Structure Type MOL
InChI Key ZKAAZFFFHXVVKM-AWCRTANDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

741.9
MW (Da)
2.86
ALogP
11
HBA
4
HBD
201.9
PSA (Ų)
0.14
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H51N7O8S
MW 741.91
Aromatic Rings 3
Heavy Atoms 52
NP-Likeness -0.98

Activity Summary

Ki 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome Macropain subunit MB1
CHEMBL4662
Ki 9.3 9.3 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16686537 10.1021/jm058289o Proteasome Macropain subunit MB1 1
16686537 10.1021/jm058289o Proteasome component C5 1
16686537 10.1021/jm058289o Cathepsin B 1
16686537 10.1021/jm058289o Proteasome Macropain subunit 1
16686537 10.1021/jm058289o Cathepsin S 1

Data from ChEMBL 36 via Core Engine