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Compound Detail

CHEMBL4174055

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CC1(c2ccc(Cl)cc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O.Cl

Basic Information

ChEMBL ID CHEMBL4174055
Phase Preclinical
Structure Type MOL
InChI Key GKYUYTZDIJOGKR-UHFFFAOYSA-N
Parent Compound CHEMBL4301717
Active Moiety CHEMBL4301717
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

468.0
MW (Da)
2.16
ALogP
6
HBA
2
HBD
99.9
PSA (Ų)
0.63
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27Cl2N5O3
MW 504.42
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.60

Activity Summary

Ki 4 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 8.05 8.05 9.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.6 6.6 250.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.52 6.52 305.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.89 5.89 1285.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29425815 10.1016/j.ejmech.2018.01.093 Unchecked 1
29425815 10.1016/j.ejmech.2018.01.093 Beta-1 adrenergic receptor 1
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