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Compound Detail

CHEMBL3740708

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CC(C)c1nc(C(=O)NC2CCN(CC3(O)CCOCC3)CC2)c2ccccn12

Basic Information

ChEMBL ID CHEMBL3740708
Phase Preclinical
Structure Type MOL
InChI Key ZYRFYKWOKBRNHT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

400.5
MW (Da)
2.19
ALogP
6
HBA
2
HBD
79.1
PSA (Ų)
0.80
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H32N4O3
MW 400.52
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.27

Activity Summary

EC50 1 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
EC50 6.84 6.84 144.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 43.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 1083.59 nM Rattus norvegicus
F 63.0 % Rattus norvegicus
T1/2 1.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26363507 10.1016/j.ejmech.2015.08.051 Rattus norvegicus 6
26363507 10.1016/j.ejmech.2015.08.051 5-hydroxytryptamine receptor 4 2
26363507 10.1016/j.ejmech.2015.08.051 Liver microsome 2
26363507 10.1016/j.ejmech.2015.08.051 Cytochrome P450 2D6 1
26363507 10.1016/j.ejmech.2015.08.051 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine