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Compound Detail

CHEMBL144238

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COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CCl)o3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL144238
Phase Preclinical
Structure Type MOL
InChI Key PFKANRGJRNXBLW-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

490.0
MW (Da)
4.33
ALogP
8
HBA
1
HBD
107.0
PSA (Ų)
0.30
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H32ClN5O4
MW 490.00
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.88

Activity Summary

Kd 3 meas. best 9.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL326
Kd 9.39 9.39 0.4 1
Alpha-1B adrenergic receptor
CHEMBL315
Kd 8.97 8.97 1.1 1
Alpha-1A adrenergic receptor
CHEMBL319
Kd 8.17 8.17 6.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9822553 10.1021/jm9810654 Alpha-1A adrenergic receptor 1
9822553 10.1021/jm9810654 Alpha-1B adrenergic receptor 1
9822553 10.1021/jm9810654 Alpha-1D adrenergic receptor 1
9822553 10.1021/jm9810654 Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine