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Compound Detail

CHEMBL155327

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c1ccc(-c2ccno2)c(NCC2=NCCN2)c1

Basic Information

ChEMBL ID CHEMBL155327
Phase Preclinical
Structure Type MOL
InChI Key LQBHYWDFUZWZET-UHFFFAOYSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

242.3
MW (Da)
1.76
ALogP
5
HBA
2
HBD
62.5
PSA (Ų)
0.86
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 C13H14N4O
MW 242.28
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -1.08

Activity Summary

EC50 3 meas. best 9.1
IC50 3 meas. best 7.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
EC50 9.1 9.1 0.8 1
Alpha-1D adrenergic receptor
CHEMBL223
EC50 8.54 8.54 2.9 1
Alpha-1B adrenergic receptor
CHEMBL232
EC50 8.43 8.43 3.7 1
Alpha-1A adrenergic receptor
CHEMBL229
IC50 7.45 7.45 35.5 1
Alpha-1D adrenergic receptor
CHEMBL223
IC50 7.42 7.42 38.0 1
Alpha-1B adrenergic receptor
CHEMBL232
IC50 6.88 6.88 131.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11844675 10.1016/s0960-894x(01)00822-8 Alpha-1A adrenergic receptor 2
11844675 10.1016/s0960-894x(01)00822-8 Alpha-1B adrenergic receptor 2
11844675 10.1016/s0960-894x(01)00822-8 Alpha-1D adrenergic receptor 2

Data from ChEMBL 36 via Core Engine