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Compound Detail

CHEMBL3605642

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COc1ccc(S(=O)(=O)N(CC(C)C)C[C@@H](O)[C@H](Cc2ccccc2)NC(=O)O[C@H]2CO[C@H]3OC[C@H](N(C)C(=O)OC(C)(C)C)[C@H]32)cc1

Basic Information

ChEMBL ID CHEMBL3605642
Phase Preclinical
Structure Type MOL
InChI Key OEJFCUWTVNZGJI-RWIUVVJRSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

691.8
MW (Da)
3.65
ALogP
10
HBA
2
HBD
153.2
PSA (Ų)
0.32
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 C34H49N3O10S
MW 691.84
Aromatic Rings 2
Heavy Atoms 48
NP-Likeness -0.23

Activity Summary

IC50 1 meas. best 7.43
Ki 1 meas. best 10.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
Ki 10.92 10.92 0.0 1
Human immunodeficiency virus 1
CHEMBL378
IC50 7.43 7.43 37.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease Ki = 0.012 nM 10.92 Inhibition of HIV1 protease 26306007
Human immunodeficiency virus 1 IC50 = 37.0 nM 7.43 Antiviral activity against HIV1 LAI infected in human MT2 cells 26306007

Literature References

PubMed DOI Target Context # Activities
26306007 10.1021/acs.jmedchem.5b00900 Human immunodeficiency virus 1 1
26306007 10.1021/acs.jmedchem.5b00900 Protease 1

Data from ChEMBL 36 via Core Engine