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Compound Detail

CHEMBL154023

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Cc1ncoc1-c1ccccc1NCC1=NCCN1

Basic Information

ChEMBL ID CHEMBL154023
Phase Preclinical
Structure Type MOL
InChI Key KUBADPQAWRUMPM-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

256.3
MW (Da)
2.06
ALogP
5
HBA
2
HBD
62.5
PSA (Ų)
0.88
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 C14H16N4O
MW 256.31
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.71

Activity Summary

IC50 3 meas. best 6.72
EC50 1 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
EC50 7.82 7.82 15.1 1
Alpha-1A adrenergic receptor
CHEMBL229
IC50 6.72 6.72 190.6 1
Alpha-1B adrenergic receptor
CHEMBL232
IC50 6.49 6.49 323.6 1
Alpha-1D adrenergic receptor
CHEMBL223
IC50 6.46 6.46 346.7 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