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Compound Detail

CHEMBL4064718

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COc1ccc(OCC2c3ccc(N4CCOCC4)cc3CCN2C(=O)c2cccc(Br)c2)cc1

Basic Information

ChEMBL ID CHEMBL4064718
Phase Preclinical
Structure Type MOL
InChI Key JRFOQXXFYASPEX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

537.5
MW (Da)
5.11
ALogP
5
HBA
0
HBD
51.2
PSA (Ų)
0.44
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29BrN2O4
MW 537.45
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.09

Activity Summary

EC50 3 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate NMDA receptor; Grin1/Grin2c
CHEMBL2096911
EC50 5.52 5.52 3000.0 1
Ionotropic glutamate receptor NMDA 1/2D
CHEMBL3038506
EC50 5.37 5.37 4300.0 1
Glutamate NMDA receptor; Grin1/Grin2b
CHEMBL2096666
EC50 5.32 5.32 4800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28586221 10.1021/acs.jmedchem.7b00239 Glutamate NMDA receptor; Grin1/Grin2c 3
28586221 10.1021/acs.jmedchem.7b00239 Glutamate NMDA receptor; Grin1/Grin2b 3
28586221 10.1021/acs.jmedchem.7b00239 Ionotropic glutamate receptor NMDA 1/2D 3

Data from ChEMBL 36 via Core Engine