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Compound Detail

CHEMBL4857918

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CN1CCN(CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL4857918
Phase Preclinical
Structure Type MOL
InChI Key QQICDAPFTVTGQB-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

480.6
MW (Da)
4.41
ALogP
6
HBA
0
HBD
45.0
PSA (Ų)
0.42
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H37FN4O2
MW 480.63
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.29

Activity Summary

Ki 4 meas. best 8.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.07 8.07 8.6 1
D(2) dopamine receptor
CHEMBL217
Ki 7.87 7.87 13.4 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.79 7.79 16.4 1
Histamine H3 receptor
CHEMBL264
Ki 6.57 6.57 270.7 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