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Compound Detail

CHEMBL4159967

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

Basic Information

ChEMBL ID CHEMBL4159967
Phase Preclinical
Structure Type MOL
InChI Key QLSJVFAAXRHHJK-UHFFFAOYSA-N
Parent Compound CHEMBL4301968
Active Moiety CHEMBL4301968
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

473.0
MW (Da)
2.30
ALogP
6
HBA
2
HBD
85.3
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 C24H30Cl2N4O4
MW 509.43
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.40

Activity Summary

Ki 4 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.7 7.7 20.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.96 6.96 109.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.57 6.57 268.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.44 6.44 366.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine