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Compound Detail

CHEMBL2419769

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COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1.Cl

Basic Information

ChEMBL ID CHEMBL2419769
Phase Preclinical
Structure Type MOL
InChI Key HLAXELILYCMGLF-RSAXXLAASA-N
Parent Compound CHEMBL3040851
Active Moiety CHEMBL3040851
8
Targets
9
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

355.4
MW (Da)
3.25
ALogP
6
HBA
1
HBD
62.1
PSA (Ų)
0.66
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 C20H22ClNO5
MW 391.85
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness 0.29

Activity Summary

Kd 5 meas. best 9.01
Ki 4 meas. best 9.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.31 9.31 0.5 1
Alpha-1D adrenergic receptor
CHEMBL326
Kd 9.01 9.01 1.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.72 8.72 1.9 1
Alpha-1A adrenergic receptor
CHEMBL319
Kd 8.71 8.485 1.9 2
Alpha-1B adrenergic receptor
CHEMBL315
Kd 8.68 8.68 2.1 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 8.59 8.59 2.6 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.54 7.54 28.8 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 6.55 6.55 281.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23902232 10.1021/jm400867d Unchecked 6
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