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Compound Detail

CHEMBL256107

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COc1ccc(S(=O)(=O)N(CC(C)C)C[C@@H](O)[C@H](Cc2ccccc2)NC(=O)C[C@H]2CO[C@H]3OCC[C@@H]23)cc1

Basic Information

ChEMBL ID CHEMBL256107
Phase Preclinical
Structure Type MOL
InChI Key ZMLZLWMYQDSDEB-VPWBKDPUSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

560.7
MW (Da)
2.83
ALogP
7
HBA
2
HBD
114.4
PSA (Ų)
0.39
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 C29H40N2O7S
MW 560.71
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.06

Activity Summary

IC50 1 meas. best 6.32
Ki 1 meas. best 9.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 9.55 9.55 0.3 1
Human immunodeficiency virus 1
CHEMBL378
IC50 6.32 6.32 480.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17635930 10.1074/jbc.m703938200 Protease 2
17635930 10.1074/jbc.m703938200 Human immunodeficiency virus 1 1
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