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Compound Detail

CHEMBL117260

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Oc1nc2cc(C#CCN3CCC(Cc4ccccc4)CC3)ccc2[nH]1

Basic Information

ChEMBL ID CHEMBL117260
Phase Preclinical
Structure Type MOL
InChI Key JJEXWPHPFZLTCU-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

345.4
MW (Da)
3.57
ALogP
3
HBA
2
HBD
52.1
PSA (Ų)
0.71
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N3O
MW 345.45
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.81

Activity Summary

IC50 4 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 1
CHEMBL2015
IC50 8.28 6.37 5.3 2
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 6.3 6.3 500.0 1
D(2) dopamine receptor
CHEMBL339
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10978188 10.1021/jm000023o Glutamate receptor ionotropic, NMDA 1 3
20692832 10.1016/j.bmcl.2010.07.043 Glutamate NMDA receptor; GRIN1/GRIN2B 2
10978188 10.1021/jm000023o Adrenergic receptor alpha-1 1
10978188 10.1021/jm000023o D(2) dopamine receptor 1
10978188 10.1021/jm000023o Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine