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Compound Detail

CHEMBL316881

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COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1

Basic Information

ChEMBL ID CHEMBL316881
Phase Preclinical
Structure Type MOL
InChI Key JQCCQHBMYRBHBD-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
3.44
ALogP
4
HBA
0
HBD
34.5
PSA (Ų)
0.72
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 C20H22N2O2
MW 322.41
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.79

Activity Summary

Ki 4 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.75 7.675 18.0 4

Pharmacokinetic Data

Parameter Value Units Species
AUC 66.5 ng.hr.mL-1 Rattus norvegicus
Cmax 54.9 nM Rattus norvegicus
T1/2 10.3 hr Rattus norvegicus
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37077395 10.1021/acsmedchemlett.3c00077 ADMET 4
12825922 10.1021/jm030030n 5-hydroxytryptamine receptor 6 1
11689074 10.1021/jm010943m 5-hydroxytryptamine receptor 6 1
15745826 10.1016/j.bmcl.2005.01.031 5-hydroxytryptamine receptor 6 1
15974573 10.1021/jm050247c 5-hydroxytryptamine receptor 6 1

Data from ChEMBL 36 via Core Engine