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Compound Detail

CHEMBL289762

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O=C1N(Cc2cccc(O)c2)[C@H](CCc2ccccc2)[C@@H](O)[C@@H](Cc2ccccc2)N1Cc1cccc(O)c1

Basic Information

ChEMBL ID CHEMBL289762
Phase Preclinical
Structure Type MOL
InChI Key YWMZEAWUKJYZAL-XWHIBYANSA-N
1
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

522.6
MW (Da)
5.51
ALogP
4
HBA
3
HBD
84.2
PSA (Ų)
0.27
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H34N2O4
MW 522.65
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness 0.09

Activity Summary

Ki 3 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 9.52 9.52 0.3 3

Pharmacokinetic Data

Parameter Value Units Species
Cmax 120.0 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9888839 10.1021/jm9803626 Human immunodeficiency virus type 1 protease 1
9888839 10.1021/jm9803626 MT2 1
9888839 10.1021/jm9803626 Rattus norvegicus 1
11831910 10.1021/jm010417v Human immunodeficiency virus type 1 protease 1
9171880 10.1021/jm970081i Human immunodeficiency virus type 1 protease 1
9171880 10.1021/jm970081i Human immunodeficiency virus type 1 (RF/HAT ISOLATE) 1

Data from ChEMBL 36 via Core Engine