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Compound Detail

CHEMBL4777303

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COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4777303
Phase Preclinical
Structure Type MOL
InChI Key YUQSQXVZLGSUAI-KXNXZCPBSA-N
Parent Compound CHEMBL4802306
Active Moiety CHEMBL4802306
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

219.3
MW (Da)
1.69
ALogP
3
HBA
1
HBD
44.5
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H18F3NO4
MW 333.31
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness 0.65

Activity Summary

EC50 6 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.72 7.715 19.0 2
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 6.56 6.555 275.4 2
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 6.53 6.53 295.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27726356 10.1021/acs.jmedchem.6b01194 5-hydroxytryptamine receptor 2C 4
27726356 10.1021/acs.jmedchem.6b01194 5-hydroxytryptamine receptor 2B 4
27726356 10.1021/acs.jmedchem.6b01194 5-hydroxytryptamine receptor 2A 4

Data from ChEMBL 36 via Core Engine