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Compound Detail

CHEMBL19576

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Oc1nc2cc(C#CCN3CCC(O)(Cc4ccc(F)cc4)CC3)ccc2[nH]1

Basic Information

ChEMBL ID CHEMBL19576
Phase Preclinical
Structure Type MOL
InChI Key UORACTXCIWIDCR-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

379.4
MW (Da)
2.83
ALogP
4
HBA
3
HBD
72.4
PSA (Ų)
0.61
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 C22H22FN3O2
MW 379.44
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.79

Activity Summary

IC50 4 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate NMDA receptor; Grin1/Grin2b
CHEMBL2096666
IC50 7.68 7.68 21.0 1
Glutamate receptor ionotropic, NMDA 2C
CHEMBL401
IC50 7.62 7.62 24.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 4.75 4.75 18000.0 1
D(2) dopamine receptor
CHEMBL339
IC50 4.39 4.39 41000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10978188 10.1021/jm000023o Glutamate receptor ionotropic, NMDA 2C 3
14980668 10.1016/j.bmcl.2003.12.049 Rattus norvegicus 2
14980668 10.1016/j.bmcl.2003.12.049 Glutamate NMDA receptor; Grin1/Grin2b 1
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