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Compound Detail

CHEMBL105267

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

Basic Information

ChEMBL ID CHEMBL105267
Phase Preclinical
Structure Type MOL
InChI Key RRBSCZCNYAJFEJ-LJQANCHMSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

321.4
MW (Da)
3.03
ALogP
4
HBA
1
HBD
62.3
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 C20H23N3O
MW 321.42
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.19

Activity Summary

Ki 4 meas. best 8.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 8.21 8.21 6.2 1
Histamine H3 receptor
CHEMBL4124
Ki 7.2 7.2 63.1 1
Histamine H2 receptor
CHEMBL1941
Ki 5.13 5.13 7413.1 1
Histamine H1 receptor
CHEMBL231
Ki 4.86 4.86 13803.8 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