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Compound Detail

CHEMBL311298

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Nc1ccc(CN2C(=O)N(Cc3ccc4[nH]ncc4c3)[C@H](Cc3ccccc3)[C@H](O)[C@@H](O)[C@H]2Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL311298
Phase Preclinical
Structure Type MOL
InChI Key WYDHHVYLPYCAIL-FYZVQMPESA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
4.53
ALogP
5
HBA
4
HBD
118.7
PSA (Ų)
0.21
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H35N5O3
MW 561.69
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -0.43

Activity Summary

Ki 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 10.52 10.52 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 10600.0 nM Canis lupus familiaris
F 100.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease Ki = 0.03 nM 10.52 Inhibitory activity against HIV protease 9632373

Literature References

PubMed DOI Target Context # Activities
9632373 10.1021/jm980103g Human immunodeficiency virus type 1 protease 4
9632373 10.1021/jm980103g MT2 1
9632373 10.1021/jm980103g ADMET 1
9632373 10.1021/jm980103g Canis familiaris 1

Data from ChEMBL 36 via Core Engine