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Compound Detail

CHEMBL4870307

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COc1cc(CN2CCCCC2)ccc1OCCCN1CCC(c2noc3cc(F)ccc23)CC1

Basic Information

ChEMBL ID CHEMBL4870307
Phase Preclinical
Structure Type MOL
InChI Key XJPIMYAKYUJUQV-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

481.6
MW (Da)
5.61
ALogP
6
HBA
0
HBD
51.0
PSA (Ų)
0.37
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36FN3O3
MW 481.61
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.33

Activity Summary

Ki 4 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.05 8.05 9.0 1
D(2) dopamine receptor
CHEMBL217
Ki 8.02 8.02 9.5 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.17 7.17 67.7 1
Histamine H3 receptor
CHEMBL264
Ki 6.59 6.59 256.0 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