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Compound Detail

CHEMBL4076286

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FC(F)(F)c1c(-c2ccc(CNC3CCOCC3)c(Cl)c2)ccn2c(CC3CC3)nnc12

Basic Information

ChEMBL ID CHEMBL4076286
Phase Preclinical
Structure Type MOL
InChI Key SCOBFXVAWLTPQZ-UHFFFAOYSA-N
1
Targets
3
Activities
3
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

464.9
MW (Da)
5.29
ALogP
5
HBA
1
HBD
51.5
PSA (Ų)
0.54
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24ClF3N4O
MW 464.92
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.04

Activity Summary

EC50 1 meas. best 6.2
Kd 1 meas. best 7.27
Ki 1 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 2
CHEMBL5137
Kd 7.27 7.27 54.0 1
Metabotropic glutamate receptor 2
CHEMBL5137
Ki 7.21 7.21 61.7 1
Metabotropic glutamate receptor 2
CHEMBL5137
EC50 6.2 6.2 631.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28704052 10.1021/acs.jmedchem.7b00669 Metabotropic glutamate receptor 2 6

Data from ChEMBL 36 via Core Engine