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Compound Detail

CHEMBL1098199

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CN(C)C(=O)NCCCc1c(CN(C)[C@H]2CCCc3cccnc32)ncc2ccccc12

Basic Information

ChEMBL ID CHEMBL1098199
Phase Preclinical
Structure Type MOL
InChI Key KEFWRLINBWLZQM-DEOSSOPVSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

431.6
MW (Da)
4.34
ALogP
4
HBA
1
HBD
61.4
PSA (Ų)
0.57
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N5O
MW 431.58
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.84

Activity Summary

IC50 1 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
IC50 7.42 7.42 38.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 16.0 mL.min-1.kg-1 Rattus norvegicus
F 20.0 % Rattus norvegicus
T1/2 3.1 hr Rattus norvegicus
Vd 1.7 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20443225 10.1016/j.bmcl.2010.03.118 Rattus norvegicus 4
20443225 10.1016/j.bmcl.2010.03.118 Human immunodeficiency virus 1 1
20443225 10.1016/j.bmcl.2010.03.118 HOS 1

Data from ChEMBL 36 via Core Engine