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Compound Detail

CHEMBL104669

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N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL104669
Phase Preclinical
Structure Type MOL
InChI Key XZKDSZJJFHAYFJ-LJQANCHMSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
3.06
ALogP
4
HBA
1
HBD
56.5
PSA (Ų)
0.83
QED
0
Ro5 Violations
6
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 2
Heavy Atoms 24
NP-Likeness -1.13

Activity Summary

Ki 4 meas. best 8.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 8.08 8.08 8.3 1
Histamine H3 receptor
CHEMBL4124
Ki 7.29 7.29 51.3 1
Histamine H1 receptor
CHEMBL231
Ki 5.35 5.35 4466.8 1
Histamine H2 receptor
CHEMBL1941
Ki 4.77 4.77 16982.4 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

Data from ChEMBL 36 via Core Engine