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Compound Detail

CHEMBL324516

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CC(C)(C)NC(=O)C1CN(Cc2cc3cccnc3o2)CCN1CC(O)CC(Cc1ccccc1)C(=O)NC1c2ccccc2CC1O

Basic Information

ChEMBL ID CHEMBL324516
Phase Preclinical
Structure Type MOL
InChI Key SIZLAJZUXGNMNI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

653.8
MW (Da)
3.61
ALogP
8
HBA
4
HBD
131.2
PSA (Ų)
0.19
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 C38H47N5O5
MW 653.82
Aromatic Rings 4
Heavy Atoms 48
NP-Likeness -0.31

Activity Summary

IC50 1 meas. best 9.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 9.49 9.49 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 1170.0 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 = 0.32 nM 9.49 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