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Compound Detail

CHEMBL4176588

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COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(C)cc3)C2=O)CC1.Cl

Basic Information

ChEMBL ID CHEMBL4176588
Phase Preclinical
Structure Type MOL
InChI Key GQGXFFRBMBQASB-UHFFFAOYSA-N
Parent Compound CHEMBL4300745
Active Moiety CHEMBL4300745
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

452.6
MW (Da)
1.95
ALogP
6
HBA
2
HBD
85.3
PSA (Ų)
0.63
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33ClN4O4
MW 489.02
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.31

Activity Summary

Ki 3 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.3 7.3 50.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.74 6.74 184.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.06 6.06 876.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29425815 10.1016/j.ejmech.2018.01.093 D(2) dopamine receptor 1
29425815 10.1016/j.ejmech.2018.01.093 5-hydroxytryptamine receptor 1A 1
29425815 10.1016/j.ejmech.2018.01.093 5-hydroxytryptamine receptor 7 1
29425815 10.1016/j.ejmech.2018.01.093 Adrenergic receptor alpha-1 1
29425815 10.1016/j.ejmech.2018.01.093 Adrenergic receptor alpha-2 1
29425815 10.1016/j.ejmech.2018.01.093 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine