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Compound Detail

CHEMBL178669

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CC(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1

Basic Information

ChEMBL ID CHEMBL178669
Phase Preclinical
Structure Type MOL
InChI Key NZJGJTYYIDLYKN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

508.6
MW (Da)
0.78
ALogP
7
HBA
1
HBD
108.5
PSA (Ų)
0.55
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H36N4O6S
MW 508.64
Aromatic Rings 1
Heavy Atoms 35
NP-Likeness -1.60

Activity Summary

Ki 1 meas. best 9.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 9.9 9.9 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 6.0 mL.min-1.kg-1 Canis lupus familiaris
F 51.0 % Canis lupus familiaris
T1/2 1.3 hr Canis lupus familiaris
T1/2 4.6 hr Canis lupus familiaris
Vd 0.7 L.kg-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 4 Ki = 0.1259 nM 9.9 Inhibitory constant for human cloned 5-HT4 receptor 15745824

Literature References

PubMed DOI Target Context # Activities
15745824 10.1016/j.bmcl.2005.01.039 ADMET 7
15745824 10.1016/j.bmcl.2005.01.039 5-hydroxytryptamine receptor 4 1

Data from ChEMBL 36 via Core Engine