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Compound Detail

CHEMBL57163

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O=c1[nH]c2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccccc2Cl)CC1

Basic Information

ChEMBL ID CHEMBL57163
Phase Preclinical
Structure Type MOL
InChI Key FKIGXRKDASCJOU-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

423.9
MW (Da)
2.65
ALogP
5
HBA
2
HBD
77.1
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22ClN5O2
MW 423.90
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.30

Activity Summary

Ki 5 meas. best 9.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 9.28 9.28 0.5 1
Alpha-1A adrenergic receptor
CHEMBL319
Ki 9.28 9.28 0.5 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 8.59 8.59 2.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1648138 10.1021/jm00110a014 Alpha-1A adrenergic receptor 1
1648138 10.1021/jm00110a014 5-hydroxytryptamine receptor 1A 1
1648138 10.1021/jm00110a014 Adrenergic receptor alpha-2 1
1648138 10.1021/jm00110a014 Beta-2 adrenergic receptor 1
12825930 10.1021/jm0307741 Alpha-1A adrenergic receptor 1
12825930 10.1021/jm0307741 Alpha-1B adrenergic receptor 1
12825930 10.1021/jm0307741 Alpha-1D adrenergic receptor 1
15801833 10.1021/jm040870h Adrenergic receptor alpha-1 1
15801833 10.1021/jm040870h 5-hydroxytryptamine receptor 1A 1
15801833 10.1021/jm040870h Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine