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Compound Detail

CHEMBL257976

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CNC(=O)c1cccc2c1CCC2c1ncc[nH]1

Basic Information

ChEMBL ID CHEMBL257976
Phase Preclinical
Structure Type MOL
InChI Key SIMGMPZLDHYMNW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

241.3
MW (Da)
1.85
ALogP
2
HBA
2
HBD
57.8
PSA (Ų)
0.84
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H15N3O
MW 241.29
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.49

Activity Summary

EC50 2 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
EC50 5.66 5.66 2200.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 5.36 5.36 4340.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18400496 10.1016/j.bmcl.2008.03.070 Alpha-1A adrenergic receptor 2
18400496 10.1016/j.bmcl.2008.03.070 Alpha-2A adrenergic receptor 2
18400496 10.1016/j.bmcl.2008.03.070 Alpha-1B adrenergic receptor 1
18400496 10.1016/j.bmcl.2008.03.070 Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine