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Compound Detail

CHEMBL2419771

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COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2.Cl

Basic Information

ChEMBL ID CHEMBL2419771
Phase Preclinical
Structure Type MOL
InChI Key RYWXHEQNEXECJD-RSAXXLAASA-N
Parent Compound CHEMBL3040800
Active Moiety CHEMBL3040800
8
Targets
9
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

357.4
MW (Da)
2.44
ALogP
6
HBA
1
HBD
58.2
PSA (Ų)
0.77
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24ClNO5
MW 393.87
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.16

Activity Summary

Kd 5 meas. best 9.58
Ki 4 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL326
Kd 9.58 9.58 0.3 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.7 8.7 2.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.65 8.65 2.2 1
Alpha-1B adrenergic receptor
CHEMBL315
Kd 8.49 8.49 3.2 1
Alpha-1A adrenergic receptor
CHEMBL319
Kd 7.88 7.675 13.2 2
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.66 7.66 21.9 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.33 7.33 46.8 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 6.63 6.63 234.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23902232 10.1021/jm400867d Unchecked 7
23902232 10.1021/jm400867d Alpha-1A adrenergic receptor 3
23902232 10.1021/jm400867d Alpha-1D adrenergic receptor 2
23902232 10.1021/jm400867d Alpha-1B adrenergic receptor 2
23902232 10.1021/jm400867d Adrenergic receptor alpha-2 1
23902232 10.1021/jm400867d 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine