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Compound Detail

CHEMBL4642338

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CC[C@@](O)(c1nnn(Cc2ccc3c(-c4ccc(F)cc4)cc(C(N)=O)nc3c2)n1)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4642338
Phase Preclinical
Structure Type MOL
InChI Key UZTDYJVVVFMAQX-OAQYLSRUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

474.4
MW (Da)
3.33
ALogP
7
HBA
2
HBD
119.8
PSA (Ų)
0.41
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18F4N6O2
MW 474.42
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.30

Activity Summary

IC50 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 2
CHEMBL5137
IC50 7.8 7.8 16.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Metabotropic glutamate receptor 2 IC50 = 16.0 nM 7.8 Negative allosteric modulation of human mGluR2 by FLIPR assay 32173198

Literature References

PubMed DOI Target Context # Activities
32173198 10.1016/j.bmcl.2020.127066 Metabotropic glutamate receptor 2 1
32173198 10.1016/j.bmcl.2020.127066 Metabotropic glutamate receptor 3 1

Data from ChEMBL 36 via Core Engine