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Compound Detail

CHEMBL4863980

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Fc1ccc2c(C3CCN(CCCOc4ccc(CN5CCOCC5)c(Cl)c4)CC3)noc2c1

Basic Information

ChEMBL ID CHEMBL4863980
Phase Preclinical
Structure Type MOL
InChI Key PMQRGOWDOYXFIQ-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

488.0
MW (Da)
5.10
ALogP
6
HBA
0
HBD
51.0
PSA (Ų)
0.41
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H31ClFN3O3
MW 488.00
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.80

Activity Summary

Ki 4 meas. best 8.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 8.27 8.27 5.4 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.2 8.2 6.3 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.82 6.82 152.2 1
Histamine H3 receptor
CHEMBL264
Ki 6.79 6.79 163.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33705900 10.1016/j.bmcl.2021.127909 D(2) dopamine receptor 1
33705900 10.1016/j.bmcl.2021.127909 5-hydroxytryptamine receptor 1A 1
33705900 10.1016/j.bmcl.2021.127909 5-hydroxytryptamine receptor 2A 1
33705900 10.1016/j.bmcl.2021.127909 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine