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Compound Detail

CHEMBL321738

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O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL321738
Phase Preclinical
Structure Type MOL
InChI Key SPTDHEOVEZUOPD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

357.9
MW (Da)
2.89
ALogP
3
HBA
1
HBD
35.6
PSA (Ų)
0.86
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 C20H24ClN3O
MW 357.88
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.76

Activity Summary

IC50 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
IC50 6.16 6.16 696.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor IC50 = 696.0 nM 6.16 Antihistaminic activity against Histamine H1 receptor was measured on isolated t... 1977909

Literature References

PubMed DOI Target Context # Activities
1977909 10.1021/jm00173a011 Histamine H1 receptor 2
- 10.1007/s00044-004-0114-7 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine