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Compound Detail

CHEMBL4279922

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COc1ccc(N2C(=O)O[C@@H]3C[C@H](OC(=O)N[C@@H](Cc4ccccc4)[C@H](O)CN(CC(C)C)S(=O)(=O)c4ccc(OC)cc4)C[C@@H]32)cc1

Basic Information

ChEMBL ID CHEMBL4279922
Phase Preclinical
Structure Type MOL
InChI Key ZCTIWAVCVCDOIV-MYOWWLDYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

681.8
MW (Da)
4.61
ALogP
9
HBA
2
HBD
143.9
PSA (Ų)
0.25
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H43N3O9S
MW 681.81
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness -0.04

Activity Summary

Ki 1 meas. best 9.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
Ki 9.2 9.2 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease Ki = 0.63 nM 9.2 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 Protease 1
30354121 10.1021/acs.jmedchem.8b01227 Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine