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Compound Detail

CHEMBL452873

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Cc1ccccc1CNC(=O)[C@H]1N(C(=O)[C@@H](O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CS(=O)(=O)c2ccc(Cl)cc2)NS(C)(=O)=O)CSC1(C)C

Basic Information

ChEMBL ID CHEMBL452873
Phase Preclinical
Structure Type MOL
InChI Key PAOJVONJUSCBHR-RRGQHJHPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

765.4
MW (Da)
2.42
ALogP
9
HBA
4
HBD
179.1
PSA (Ų)
0.19
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 C34H41ClN4O8S3
MW 765.38
Aromatic Rings 3
Heavy Atoms 50
NP-Likeness -0.49

Activity Summary

IC50 1 meas. best 9.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
IC50 9.96 9.96 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease IC50 = 0.11 nM 9.96 Inhibition of HIV1 protease 18426195

Literature References

PubMed DOI Target Context # Activities
18426195 10.1021/jm701555p Protease 2
18426195 10.1021/jm701555p Human immunodeficiency virus 1 1
18426195 10.1021/jm701555p MT4 1
18426195 10.1021/jm701555p Unchecked 1

Data from ChEMBL 36 via Core Engine