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Compound Detail

CHEMBL4861643

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CC1CCN(CCc2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL4861643
Phase Preclinical
Structure Type MOL
InChI Key CRMAPALWSALKCW-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

493.7
MW (Da)
6.28
ALogP
5
HBA
0
HBD
41.7
PSA (Ų)
0.31
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H40FN3O2
MW 493.67
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.15

Activity Summary

Ki 4 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 8.57 8.57 2.7 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 8.36 8.36 4.4 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.29 8.29 5.1 1
Histamine H3 receptor
CHEMBL264
Ki 7.8 7.8 15.8 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