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Compound Detail

CHEMBL319000

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CN(C)[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1

Basic Information

ChEMBL ID CHEMBL319000
Phase Preclinical
Structure Type MOL
InChI Key FXIPXWLVYIHFEP-OAQYLSRUSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

349.5
MW (Da)
3.63
ALogP
4
HBA
0
HBD
39.5
PSA (Ų)
0.72
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 C22H27N3O
MW 349.48
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.43

Activity Summary

Ki 6 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 8.7 8.5533 2.0 3
Histamine H3 receptor
CHEMBL4124
Ki 7.87 7.87 13.5 1
Histamine H1 receptor
CHEMBL231
Ki 5.72 5.72 1905.5 1
Histamine H2 receptor
CHEMBL1941
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12372505 10.1016/s0960-894x(02)00648-0 Histamine H3 receptor 2
12372505 10.1016/s0960-894x(02)00648-0 Histamine H1 receptor 1
12372505 10.1016/s0960-894x(02)00648-0 Histamine H2 receptor 1
19456097 10.1021/jm900409x Histamine H3 receptor 1
33261900 10.1016/j.ejmech.2020.113041 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine