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Compound Detail

CHEMBL325527

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O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@@H]1CCOC1)OCc1ccccn1

Basic Information

ChEMBL ID CHEMBL325527
Phase Preclinical
Structure Type MOL
InChI Key AAGQNDDFCSYHQM-DDOVKQMLSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

652.8
MW (Da)
5.05
ALogP
8
HBA
4
HBD
148.1
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 C37H40N4O7
MW 652.75
Aromatic Rings 4
Heavy Atoms 48
NP-Likeness -0.27

Activity Summary

EC50 1 meas. best 7.52
Ki 1 meas. best 10.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 10.4 10.4 0.0 1
CCRF-CEM
CHEMBL382
EC50 7.52 7.52 30.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 1037.0 nM Rattus norvegicus
F 6.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9934467 10.1016/s0960-894x(98)00657-x Rattus norvegicus 2
9934467 10.1016/s0960-894x(98)00657-x Human immunodeficiency virus type 1 protease 1
9934467 10.1016/s0960-894x(98)00657-x CCRF-CEM 1

Data from ChEMBL 36 via Core Engine