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Compound Detail

CHEMBL4469549

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COc1ccc(S(=O)(=O)N(CC(C)C)C[C@@H](O)[C@H](Cc2ccccc2)NC(=O)O[C@H]2C[C@H]3CO[C@H]4OC2C[C@@H]34)cc1

Basic Information

ChEMBL ID CHEMBL4469549
Phase Preclinical
Structure Type MOL
InChI Key NEABZPBSTVJYAP-IKKXBQPXSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

588.7
MW (Da)
3.19
ALogP
8
HBA
2
HBD
123.6
PSA (Ų)
0.39
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H40N2O8S
MW 588.72
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness 0.29

Activity Summary

IC50 1 meas. best 7.14
Ki 1 meas. best 10.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
Ki 10.47 10.47 0.0 1
Human immunodeficiency virus 1
CHEMBL378
IC50 7.14 7.14 71.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease Ki = 0.034 nM 10.47 Inhibition of HIV-1 protease 32348139
Human immunodeficiency virus 1 IC50 = 71.7 nM 7.14 Antiviral activity against HIV1 LAI infected in human MT2 cells 32348139

Literature References

PubMed DOI Target Context # Activities
32348139 10.1021/acs.jmedchem.0c00202 Protease 1
32348139 10.1021/acs.jmedchem.0c00202 Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine