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Compound Detail

CHEMBL364376

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O=C(N[C@H]1CCOC[C@H]1O)[C@H](Cc1nnc(-c2ccccc2)o1)C[C@H](O)CN1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)C[C@H]1C(=O)NCC(F)(F)F

Basic Information

ChEMBL ID CHEMBL364376
Phase Preclinical
Structure Type MOL
InChI Key QRGSOTVIQOYHBA-KPMWDHBHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

775.2
MW (Da)
3.69
ALogP
11
HBA
4
HBD
166.4
PSA (Ų)
0.15
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 C37H42ClF3N6O7
MW 775.23
Aromatic Rings 4
Heavy Atoms 54
NP-Likeness -0.99

Activity Summary

IC50 1 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 11.0 11.0 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease IC50 = 0.01 nM 11.0 Inhibitory concentration against HIV-1 protease (NL4-3) 15324882

Literature References

PubMed DOI Target Context # Activities
15324882 10.1016/j.bmcl.2004.06.092 MT4 5
15324882 10.1016/j.bmcl.2004.06.092 Human immunodeficiency virus type 1 protease 1

Data from ChEMBL 36 via Core Engine