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Compound Detail

CHEMBL132231

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COc1cc(CN2C(=O)N(Cc3cccc(C(=O)Nc4cnccn4)c3)[C@H](Cc3ccccc3)[C@H](O)[C@@H](O)[C@H]2Cc2ccccc2)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL132231
Phase Preclinical
Structure Type MOL
InChI Key AKQVVKQZOJNELV-PASMDFPHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

687.8
MW (Da)
5.13
ALogP
8
HBA
3
HBD
137.3
PSA (Ų)
0.16
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 C40H41N5O6
MW 687.80
Aromatic Rings 5
Heavy Atoms 51
NP-Likeness -0.55

Activity Summary

Ki 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 8.6 8.6 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease Ki = 2.511 nM 8.6 Affinity against HIV protease 9406598

Literature References

PubMed DOI Target Context # Activities
9406598 10.1021/jm970288b Human immunodeficiency virus type 1 protease 2
9406598 10.1021/jm970288b No relevant target 1

Data from ChEMBL 36 via Core Engine