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Compound Detail

CHEMBL280303

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Cn1cnc(S(=O)(=O)Nc2cccc([C@@H](c3c(O)c4c(oc3=O)CCCCCC4)C3CC3)c2)c1

Basic Information

ChEMBL ID CHEMBL280303
Phase Preclinical
Structure Type MOL
InChI Key CSUKPQVMRKQBSB-QFIPXVFZSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
5
Publications
0
Known Names

Molecular Properties

483.6
MW (Da)
4.08
ALogP
7
HBA
2
HBD
114.4
PSA (Ų)
0.55
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N3O5S
MW 483.59
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.57

Activity Summary

Ki 1 meas. best 10.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 10.35 10.35 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 19.0 - Rattus norvegicus
AUC 6.0 - Rattus norvegicus
CL 4.667 mL.min-1.kg-1 Rattus norvegicus
Cmax 640.0 nM Rattus norvegicus
F 15.0 % Rattus norvegicus
T1/2 2.4 hr Rattus norvegicus
Tmax 0.25 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 = 0.045 nM 10.35 Binding affinity against HIV-1 protease 9089336

Literature References

PubMed DOI Target Context # Activities
9089336 10.1021/jm960441m Rattus norvegicus 7
9089336 10.1021/jm960441m Human immunodeficiency virus type 1 protease 1
9089336 10.1021/jm960441m Human immunodeficiency virus 1 1
9089336 10.1021/jm960441m H9 1
9089336 10.1021/jm960441m ADMET 1

Data from ChEMBL 36 via Core Engine