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Compound Detail

CHEMBL509387

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CC[C@]12CCCN3CC[C@]4(C(=C(C(=O)OC)C1)Nc1ccccc14)[C@@H]32.Cl

Basic Information

ChEMBL ID CHEMBL509387
Phase Preclinical
Structure Type MOL
InChI Key BFVXDLZRORZNHX-OCIDDWSYSA-N
Parent Compound CHEMBL251690
Active Moiety CHEMBL251690
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
3.45
ALogP
4
HBA
1
HBD
41.6
PSA (Ų)
0.84
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27ClN2O2
MW 374.91
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness 1.83

Activity Summary

Ki 3 meas. best 5.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.38 5.38 4200.0 1
Unchecked
CHEMBL612545
Ki 5.33 5.33 4650.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 5.29 5.29 5100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9182127 10.1021/np960482l Unchecked 9
9182127 10.1021/np960482l 5-hydroxytryptamine receptor 1A 1
9182127 10.1021/np960482l 5-hydroxytryptamine receptor 2A 1
9182127 10.1021/np960482l 5-hydroxytryptamine receptor 3A 1
9182127 10.1021/np960482l D(1A) dopamine receptor 1
9182127 10.1021/np960482l D(2) dopamine receptor 1
9182127 10.1021/np960482l Histamine H1 receptor 1
9182127 10.1021/np960482l Glucocorticoid receptor 1
9182127 10.1021/np960482l Adrenergic receptor alpha-1 1
9182127 10.1021/np960482l Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine