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Compound Detail

CHEMBL16584

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O=c1c2c(oc(O)c1C(c1ccccc1)C1CC1)CCCCCC2

Basic Information

ChEMBL ID CHEMBL16584
Phase Preclinical
Structure Type MOL
InChI Key KJZFBVIJZBENEN-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
10
PK Parameters
4
Publications
0
Known Names

Molecular Properties

324.4
MW (Da)
4.55
ALogP
3
HBA
1
HBD
50.4
PSA (Ų)
0.90
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24O3
MW 324.42
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness 0.10

Activity Summary

Ki 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 7.82 7.42 15.0 2
Human rhinovirus A protease
CHEMBL2857
Ki 7.82 7.82 15.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 374.0 - Rattus norvegicus
AUC 388.0 - Rattus norvegicus
CL 0.65 mL.min-1.kg-1 Rattus norvegicus
Cmax 40800.0 nM Rattus norvegicus
Cmax 30300.0 nM Rattus norvegicus
F 91.0 % Rattus norvegicus
F 99.0 % Rattus norvegicus
T1/2 4.9 hr Rattus norvegicus
Tmax 3.7 hr Rattus norvegicus
Tmax 6.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7783120 10.1021/jm00011a008 Rattus norvegicus 11
7783120 10.1021/jm00011a008 Human rhinovirus A protease 2
7473573 10.1021/jm00022a011 Human immunodeficiency virus type 1 protease 1
9089336 10.1021/jm960441m Human immunodeficiency virus type 1 protease 1

Data from ChEMBL 36 via Core Engine