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Compound Detail

CHEMBL4537236

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O=C1N[C@H](c2cncc(C#Cc3ccccc3)c2)[C@@H](c2ccccc2F)O1

Basic Information

ChEMBL ID CHEMBL4537236
Phase Preclinical
Structure Type MOL
InChI Key RETSDKVSYUCURH-NHCUHLMSSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

358.4
MW (Da)
4.14
ALogP
3
HBA
1
HBD
51.2
PSA (Ų)
0.70
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H15FN2O2
MW 358.37
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.52

Activity Summary

EC50 1 meas. best 8.82
Ki 1 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 5
CHEMBL3227
EC50 8.82 8.82 1.5 1
Metabotropic glutamate receptor 5
CHEMBL3227
Ki 8.72 8.72 1.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27496211 10.1016/j.bmcl.2016.07.065 Metabotropic glutamate receptor 5 4

Data from ChEMBL 36 via Core Engine