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Compound Detail

CHEMBL4784475

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CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)[C@H]1CO[C@H]2OCC[C@H]21)S(=O)(=O)c1ccc2nc(NC3CC3)sc2c1

Basic Information

ChEMBL ID CHEMBL4784475
Phase Preclinical
Structure Type MOL
InChI Key QULGQKLQPRYULA-QETJVHQUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

656.9
MW (Da)
4.25
ALogP
9
HBA
3
HBD
130.1
PSA (Ų)
0.23
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 C33H44N4O6S2
MW 656.87
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.65

Activity Summary

Ki 1 meas. best 6.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 6.55 6.55 284.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease Ki = 284.0 nM 6.55 Inhibition of HIV1 protease by fluorescence based assay 33062180

Literature References

PubMed DOI Target Context # Activities
33062180 10.1021/acsmedchemlett.9b00670 Human immunodeficiency virus type 1 protease 1
33062180 10.1021/acsmedchemlett.9b00670 Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine