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Compound Detail

CHEMBL3410210

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Cc1ccc(C#Cc2ncn3c2COc2ccccc2-3)cc1

Basic Information

ChEMBL ID CHEMBL3410210
Phase Preclinical
Structure Type MOL
InChI Key KYFAZBYUDNHGIY-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

286.3
MW (Da)
3.47
ALogP
3
HBA
0
HBD
27.1
PSA (Ų)
0.59
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14N2O
MW 286.33
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 5.25
Ki 1 meas. best 5.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 5
CHEMBL3227
Ki 5.55 5.55 2840.0 1
Metabotropic glutamate receptor 5
CHEMBL3227
IC50 5.25 5.25 5600.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 161.0 mL.min-1.g-1 Rattus norvegicus
CL 32.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25565255 10.1021/jm501642c Metabotropic glutamate receptor 5 2
25565255 10.1021/jm501642c Liver microsome 2
25565255 10.1021/jm501642c GABA-A receptor; anion channel 1

Data from ChEMBL 36 via Core Engine