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Compound Detail

CHEMBL431306

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O=C1N(CC2CC2)[C@H](Cc2ccccc2)[C@H](O)[C@@H](O)[C@@H](Cc2ccccc2)N1CC1CC1

Basic Information

ChEMBL ID CHEMBL431306
Phase Preclinical
Structure Type MOL
InChI Key YMTOUOZOBVYCFQ-XPGKHFPBSA-N

Known Names

XK-234
1
Targets
5
Activities
1
Assay Types
4
PK Parameters
13
Publications
1
Known Names

Molecular Properties

434.6
MW (Da)
3.49
ALogP
3
HBA
2
HBD
64.0
PSA (Ų)
0.67
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H34N2O3
MW 434.58
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness 0.09

Activity Summary

Ki 5 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 8.72 8.696 1.9 5

Pharmacokinetic Data

Parameter Value Units Species
Cmax 4300.0 nM Rattus norvegicus
Cmax 9200.0 nM Canis lupus familiaris
F 100.0 % Rattus norvegicus
F 48.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9003516 10.1021/jm960586t Human immunodeficiency virus 6
9003516 10.1021/jm960586t Human immunodeficiency virus type 1 protease 2
8667359 10.1021/jm960083n Human immunodeficiency virus type 1 protease 2
8784449 10.1021/jm9602571 ADMET 2
9003516 10.1021/jm960586t Unchecked 1
8667359 10.1021/jm960083n Human immunodeficiency virus 1 1
9554878 10.1021/jm970524i Human immunodeficiency virus type 1 protease 1
9554878 10.1021/jm970524i Human immunodeficiency virus 1 1
8784449 10.1021/jm9602571 Human immunodeficiency virus type 1 protease 1
8784449 10.1021/jm9602571 Human immunodeficiency virus 1 1
8784449 10.1021/jm9602571 Rattus norvegicus 1
8784449 10.1021/jm9602571 Canis familiaris 1
9925730 10.1021/jm980369n Human immunodeficiency virus type 1 protease 1

Data from ChEMBL 36 via Core Engine