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Compound Detail

CHEMBL4171652

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COc1ccc(C2(C)NC(=O)N(CC(O)CN3CCN(c4ccccc4C#N)CC3)C2=O)cc1.Cl

Basic Information

ChEMBL ID CHEMBL4171652
Phase Preclinical
Structure Type MOL
InChI Key RKJCOBOHNHRAJW-UHFFFAOYSA-N
Parent Compound CHEMBL4301757
Active Moiety CHEMBL4301757
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

463.5
MW (Da)
1.52
ALogP
7
HBA
2
HBD
109.1
PSA (Ų)
0.60
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 C25H30ClN5O4
MW 500.00
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.39

Activity Summary

Ki 3 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.64 7.64 23.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.66 6.66 219.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.11 6.11 782.0 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