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Compound Detail

CHEMBL3416063

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C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN.Cl

Basic Information

ChEMBL ID CHEMBL3416063
Phase Preclinical
Structure Type MOL
InChI Key MNIAWGCBQVLINM-XQKZEKTMSA-N
Parent Compound CHEMBL3546958
Active Moiety CHEMBL3546958
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

221.3
MW (Da)
2.45
ALogP
2
HBA
1
HBD
35.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H17ClFNO
MW 257.74
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.21

Activity Summary

EC50 2 meas. best 8.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 8.38 8.38 4.2 1
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 6.43 6.43 374.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25633969 10.1021/jm5019274 Voltage-gated inwardly rectifying potassium channel KCNH2 6
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2A 2
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2C 2
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 6 1
25633969 10.1021/jm5019274 Cytochrome P450 3A4 1
25633969 10.1021/jm5019274 Unchecked 1
25633969 10.1021/jm5019274 Mus musculus 1
25633969 10.1021/jm5019274 D(3) dopamine receptor 1
25633969 10.1021/jm5019274 Alpha-2C adrenergic receptor 1
25633969 10.1021/jm5019274 Alpha-2B adrenergic receptor 1
25633969 10.1021/jm5019274 Alpha-2A adrenergic receptor 1
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 7 1
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 1A 1
25633969 10.1021/jm5019274 Cytochrome P450 2B6 1
25633969 10.1021/jm5019274 Cytochrome P450 2C19 1
25633969 10.1021/jm5019274 Cytochrome P450 2C9 1
25633969 10.1021/jm5019274 Cytochrome P450 2D6 1
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2B 1

Data from ChEMBL 36 via Core Engine