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Compound Detail

CHEMBL4064935

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COc1ccc(F)cc1C1CC1CNCc1cccc2cccnc12.Cl

Basic Information

ChEMBL ID CHEMBL4064935
Phase Preclinical
Structure Type MOL
InChI Key CZQBVUQTVSEYGC-UHFFFAOYSA-N
Parent Compound CHEMBL4116446
Active Moiety CHEMBL4116446
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

336.4
MW (Da)
4.28
ALogP
3
HBA
1
HBD
34.1
PSA (Ų)
0.73
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22ClFN2O
MW 372.87
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.69

Activity Summary

EC50 6 meas. best 7.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.06 7.06 87.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 6.34 6.34 457.1 2
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 6.28 6.28 524.8 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

Data from ChEMBL 36 via Core Engine