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Compound Detail

CHEMBL537651

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Cl.Cl.c1ccc2c(C3CCN(CCCCCN4CCCCC4)CC3)c[nH]c2c1

Basic Information

ChEMBL ID CHEMBL537651
Phase Preclinical
Structure Type MOL
InChI Key MZDFHYLRHMOQGE-UHFFFAOYSA-N
Parent Compound CHEMBL1188902
Active Moiety CHEMBL1188902
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

353.6
MW (Da)
5.00
ALogP
2
HBA
1
HBD
22.3
PSA (Ų)
0.71
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H37Cl2N3
MW 426.48
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.61

Activity Summary

Ki 4 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1B adrenergic receptor
CHEMBL315
Ki 8.82 8.82 1.5 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.43 7.43 37.0 1
Alpha-1A adrenergic receptor
CHEMBL319
Ki 7.24 7.24 57.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 6.45 6.45 355.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16723224 10.1016/j.bmcl.2006.05.002 Adrenergic receptor beta 1
16723224 10.1016/j.bmcl.2006.05.002 Adrenergic receptor alpha-2 1
16723224 10.1016/j.bmcl.2006.05.002 Alpha-1D adrenergic receptor 1
16723224 10.1016/j.bmcl.2006.05.002 Alpha adrenergic receptor 1A and 1B 1
16723224 10.1016/j.bmcl.2006.05.002 Alpha-1B adrenergic receptor 1
16723224 10.1016/j.bmcl.2006.05.002 Alpha-1A adrenergic receptor 1

Data from ChEMBL 36 via Core Engine