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Compound Detail

CHEMBL4286215

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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]3OC(=O)N(c4ccccc4)[C@H]3C2)cc1

Basic Information

ChEMBL ID CHEMBL4286215
Phase Preclinical
Structure Type MOL
InChI Key MCFYAJCOYWLLEO-YGMVDIOKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

651.8
MW (Da)
4.60
ALogP
8
HBA
2
HBD
134.7
PSA (Ų)
0.27
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 C34H41N3O8S
MW 651.78
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.04

Activity Summary

Ki 1 meas. best 9.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
Ki 9.48 9.48 0.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease Ki = 0.33 nM 9.48 Inhibition of HIV1 wild type NL4-3 protease expressed in Escherichia coli Rosett... 30354121

Literature References

PubMed DOI Target Context # Activities
30354121 10.1021/acs.jmedchem.8b01227 Human immunodeficiency virus 1 1
30354121 10.1021/acs.jmedchem.8b01227 Protease 1

Data from ChEMBL 36 via Core Engine