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Compound Detail

CHEMBL544243

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CC(=O)c1ccc(OCc2ccc(CN3CCCCCC3)cc2)cc1.Cl

Basic Information

ChEMBL ID CHEMBL544243
Phase Preclinical
Structure Type MOL
InChI Key JTIIPPNQSNPJSH-UHFFFAOYSA-N
Parent Compound CHEMBL1192922
Active Moiety CHEMBL1192922
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

337.5
MW (Da)
4.84
ALogP
3
HBA
0
HBD
29.5
PSA (Ų)
0.71
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 C22H28ClNO2
MW 373.92
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.94

Activity Summary

Kd 1 meas. best 7.51
Ki 1 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL5076
Kd 7.51 7.51 30.9 1
Histamine H3 receptor
CHEMBL264
Ki 7.43 7.43 37.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12672253 10.1021/jm021084k Histamine H3 receptor 3

Data from ChEMBL 36 via Core Engine