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Compound Detail

CHEMBL299514

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Cc1c(O)cccc1C(=O)N[C@@H](Cc1ccccc1)[C@H](O)C(=O)N1CSC[C@H]1C(=O)NC(C)(C)C

Basic Information

ChEMBL ID CHEMBL299514
Phase Preclinical
Structure Type MOL
InChI Key DBZLZNFYSDUNIS-ONTIZHBOSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

499.6
MW (Da)
2.22
ALogP
6
HBA
4
HBD
119.0
PSA (Ų)
0.46
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N3O5S
MW 499.63
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.41

Activity Summary

Ki 1 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 7.6 7.6 24.9 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 2910.0 nM Rattus norvegicus
F 33.9 % Rattus norvegicus
Tmax 0.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease Ki = 24.9 nM 7.6 Inhibition of recombinant HIV-1 protease (NY-5) 10346931

Literature References

PubMed DOI Target Context # Activities
10346931 10.1021/jm980637h Human immunodeficiency virus type 1 protease 3
10346931 10.1021/jm980637h Rattus norvegicus 3
10346931 10.1021/jm980637h CEM-SS 2
10346931 10.1021/jm980637h ADMET 1

Data from ChEMBL 36 via Core Engine