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Compound Detail

CHEMBL61120

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NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL61120
Phase Preclinical
Structure Type MOL
InChI Key SZCLNIBNFBNHIY-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

359.5
MW (Da)
1.54
ALogP
5
HBA
1
HBD
75.9
PSA (Ų)
0.53
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H29N3O3
MW 359.47
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness -1.15

Activity Summary

Ki 3 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL4124
Ki 9.3 9.3 0.5 1
Histamine H1 receptor
CHEMBL231
Ki 4.55 4.55 28183.8 1
Histamine H2 receptor
CHEMBL1941
Ki 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 46.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12113836 10.1016/s0960-894x(02)00310-4 Histamine H3 receptor 1
12113836 10.1016/s0960-894x(02)00310-4 Histamine H1 receptor 1
12113836 10.1016/s0960-894x(02)00310-4 Histamine H2 receptor 1
12113836 10.1016/s0960-894x(02)00310-4 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine