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Compound Detail

CHEMBL180835

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O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C3CCCC3)CC2)CC1)c1cccc2c1OCCO2

Basic Information

ChEMBL ID CHEMBL180835
Phase Preclinical
Structure Type MOL
InChI Key RXJPERJYABKLTI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

534.7
MW (Da)
2.18
ALogP
7
HBA
1
HBD
91.4
PSA (Ų)
0.52
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H42N4O5S
MW 534.72
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness -1.51

Activity Summary

Ki 1 meas. best 10.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 10.8 10.8 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 37.0 mL.min-1.kg-1 Canis lupus familiaris
F 42.0 % Canis lupus familiaris
T1/2 2.9 hr Canis lupus familiaris
Vd 9.3 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 = 0.01585 nM 10.8 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 6
15745824 10.1016/j.bmcl.2005.01.039 5-hydroxytryptamine receptor 4 1

Data from ChEMBL 36 via Core Engine