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Compound Detail

CHEMBL2206449

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COc1c(F)ccc(F)c1C1CCN(c2ccn3c(CC4CC4)nnc3c2C(F)(F)F)CC1

Basic Information

ChEMBL ID CHEMBL2206449
Phase Preclinical
Structure Type MOL
InChI Key AREDGFWKVCUPTH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

466.4
MW (Da)
5.37
ALogP
5
HBA
0
HBD
42.7
PSA (Ų)
0.47
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23F5N4O
MW 466.45
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.01

Activity Summary

EC50 1 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 2
CHEMBL5137
EC50 8.39 8.39 4.1 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.01 - Rattus norvegicus
Fu 0.01 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22992024 10.1021/jm300912k Unchecked 7
22992024 10.1021/jm300912k Liver microsomes 4
22992024 10.1021/jm300912k Metabotropic glutamate receptor 2 2
22992024 10.1021/jm300912k Plasma 2

Data from ChEMBL 36 via Core Engine