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Compound Detail

CHEMBL414774

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Cc1cc(C)c(NC(CS(=O)(=O)c2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)[C@H](O)C(=O)N2CSC(C)(C)[C@H]2C(=O)NCc2ccccc2C)c(C)c1

Basic Information

ChEMBL ID CHEMBL414774
Phase Preclinical
Structure Type MOL
InChI Key JJRQUZOWWLBKFJ-BFYLVXCISA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

821.1
MW (Da)
6.41
ALogP
8
HBA
4
HBD
144.9
PSA (Ų)
0.10
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H52N4O6S2
MW 821.08
Aromatic Rings 5
Heavy Atoms 58
NP-Likeness -0.30

Activity Summary

EC50 1 meas. best 7.21
IC50 1 meas. best 10.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 10.08 10.08 0.1 1
Human immunodeficiency virus 1
CHEMBL378
EC50 7.21 7.21 61.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.083 nM 10.08 Inhibition of HIV protease 17537628
Human immunodeficiency virus 1 EC50 = 61.0 nM 7.21 Antiviral activity against HIV1 3B in MT4 cells by MTT assay 17537628

Literature References

PubMed DOI Target Context # Activities
17537628 10.1016/j.bmcl.2007.05.039 Unchecked 3
17537628 10.1016/j.bmcl.2007.05.039 Human immunodeficiency virus 1 1
17537628 10.1016/j.bmcl.2007.05.039 MT4 1

Data from ChEMBL 36 via Core Engine