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Compound Detail

CHEMBL325395

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CC(C)(C)NC(=O)C1CN(Cc2c[nH]c3ccccc23)CCN1CC(O)CC(Cc1ccccc1)C(=O)NC1c2ccccc2CC1O

Basic Information

ChEMBL ID CHEMBL325395
Phase Preclinical
Structure Type MOL
InChI Key ZAFZTRIEIZFEAR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

651.9
MW (Da)
3.95
ALogP
6
HBA
5
HBD
120.9
PSA (Ų)
0.17
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H49N5O4
MW 651.85
Aromatic Rings 4
Heavy Atoms 48
NP-Likeness -0.26

Activity Summary

IC50 1 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 8.77 8.77 1.7 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax - nM 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 IC50 = 1.7 nM 8.77 Inhibition of HIV-1 protease in vitro. 10978186

Literature References

PubMed DOI Target Context # Activities
10978186 10.1021/jm9903848 Human immunodeficiency virus type 1 protease 2
10978186 10.1021/jm9903848 No relevant target 2
10978186 10.1021/jm9903848 Canis familiaris 2

Data from ChEMBL 36 via Core Engine