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Compound Detail

CHEMBL3938796

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Fc1ccc(C2CCN(Cc3ccn4c(CC5CC5)nnc4c3C(F)(F)F)CC2)c(F)c1

Basic Information

ChEMBL ID CHEMBL3938796
Phase Preclinical
Structure Type MOL
InChI Key CRUGMDQKVDVGOQ-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

450.5
MW (Da)
5.36
ALogP
4
HBA
0
HBD
33.4
PSA (Ų)
0.49
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 C23H23F5N4
MW 450.46
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.37

Activity Summary

EC50 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 2
CHEMBL5137
EC50 7.82 7.3167 15.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27579727 10.1021/acs.jmedchem.6b00913 Metabotropic glutamate receptor 2 2
27579727 10.1021/acs.jmedchem.6b00913 No relevant target 2
27579727 10.1021/acs.jmedchem.6b00913 ADMET 2
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 2 2
27579727 10.1021/acs.jmedchem.6b00913 Voltage-gated inwardly rectifying potassium channel KCNH2 1
35802702 10.1021/acs.jmedchem.2c00593 No relevant target 1
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 3 1
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 1 1
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 4 1
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 5 1
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 6 1
35802702 10.1021/acs.jmedchem.2c00593 Metabotropic glutamate receptor 8 1

Data from ChEMBL 36 via Core Engine