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Compound Detail

CHEMBL262642

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O=C(Nc1cnccn1)c1cccc(CN2C(=O)N(Cc3cccc(C(=O)Nc4cnccn4)c3)[C@H](Cc3ccccc3)[C@H](O)[C@@H](O)[C@H]2Cc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL262642
Phase Preclinical
Structure Type MOL
InChI Key JIICMIOQFYIENG-JFDQHVTASA-N
1
Targets
4
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

748.8
MW (Da)
5.15
ALogP
9
HBA
4
HBD
173.8
PSA (Ų)
0.13
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H40N8O5
MW 748.84
Aromatic Rings 6
Heavy Atoms 56
NP-Likeness -0.47

Activity Summary

Ki 4 meas. best 10.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 10.74 10.73 0.0 4

Pharmacokinetic Data

Parameter Value Units Species
CL 46.67 mL.min-1.kg-1 Canis lupus familiaris
Cmax 534.16 nM Canis lupus familiaris
T1/2 0.8 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9406598 10.1021/jm970288b Canis familiaris 4
9406598 10.1021/jm970288b Human immunodeficiency virus type 1 protease 2
8863807 10.1021/jm9602773 Human immunodeficiency virus type 1 protease 2
9925730 10.1021/jm980369n Human immunodeficiency virus type 1 protease 1
8863807 10.1021/jm9602773 Human immunodeficiency virus 1 1
8863807 10.1021/jm9602773 No relevant target 1

Data from ChEMBL 36 via Core Engine