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Compound Detail

CHEMBL1767161

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O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL1767161
Phase Preclinical
Structure Type MOL
InChI Key QLOCEFPHCAKSLE-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

655.3
MW (Da)
8.34
ALogP
6
HBA
0
HBD
50.6
PSA (Ų)
0.14
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H51ClN4O2
MW 655.33
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.95

Activity Summary

Ki 4 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 8.7 8.7 2.0 1
Histamine H1 receptor
CHEMBL231
Ki 7.7 7.7 19.9 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.0 7.0 100.0 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.8 6.8 158.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21381763 10.1021/jm1013874 Alpha-1B adrenergic receptor 1
21381763 10.1021/jm1013874 Alpha-1A adrenergic receptor 1
21381763 10.1021/jm1013874 Histamine H3 receptor 1
21381763 10.1021/jm1013874 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine