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Compound Detail

CHEMBL420683

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c1ccc(-c2ccccc2OCC2=NCCN2)nc1

Basic Information

ChEMBL ID CHEMBL420683
Phase Preclinical
Structure Type MOL
InChI Key FVHLKYRSFYIRKU-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

253.3
MW (Da)
2.13
ALogP
4
HBA
1
HBD
46.5
PSA (Ų)
0.91
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N3O
MW 253.31
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.80

Activity Summary

IC50 3 meas. best 6.94
EC50 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
EC50 7.9 7.9 12.6 2
Alpha-1A adrenergic receptor
CHEMBL229
IC50 6.94 6.94 114.8 1
Alpha-1D adrenergic receptor
CHEMBL223
IC50 5.95 5.95 1122.0 1
Alpha-1B adrenergic receptor
CHEMBL232
IC50 5.69 5.69 2041.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11814822 10.1016/s0960-894x(01)00764-8 Alpha-1A adrenergic receptor 3
11814822 10.1016/s0960-894x(01)00764-8 Alpha-1B adrenergic receptor 3
11814822 10.1016/s0960-894x(01)00764-8 Alpha-1D adrenergic receptor 3
12419381 10.1016/s0960-894x(02)00753-9 Alpha-1A adrenergic receptor 2
12419381 10.1016/s0960-894x(02)00753-9 Alpha-1B adrenergic receptor 1
12419381 10.1016/s0960-894x(02)00753-9 Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine