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Compound Detail

CHEMBL4086286

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COc1ccc(F)cc1C1CC1CNCc1ccccc1OCCF.Cl

Basic Information

ChEMBL ID CHEMBL4086286
Phase Preclinical
Structure Type MOL
InChI Key WJBXLZWYTOSQRC-UHFFFAOYSA-N
Parent Compound CHEMBL4117192
Active Moiety CHEMBL4117192
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

347.4
MW (Da)
4.08
ALogP
3
HBA
1
HBD
30.5
PSA (Ų)
0.74
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24ClF2NO2
MW 383.87
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.55

Activity Summary

EC50 6 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.55 7.55 28.0 2
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.25 7.25 56.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 6.4 6.4 398.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28657744 10.1021/acs.jmedchem.7b00584 5-hydroxytryptamine receptor 2A 3
28657744 10.1021/acs.jmedchem.7b00584 5-hydroxytryptamine receptor 2B 3
28657744 10.1021/acs.jmedchem.7b00584 5-hydroxytryptamine receptor 2C 3
28657744 10.1021/acs.jmedchem.7b00584 Unchecked 1

Data from ChEMBL 36 via Core Engine