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Compound Detail

CHEMBL3216590

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COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2.Cl.Cl

Basic Information

ChEMBL ID CHEMBL3216590
Phase Preclinical
Structure Type MOL
InChI Key WNDMPEJJAWXNBF-CKUXDGONSA-N
Parent Compound CHEMBL3040803
Active Moiety CHEMBL3040803
8
Targets
9
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

356.4
MW (Da)
2.47
ALogP
6
HBA
2
HBD
61.0
PSA (Ų)
0.74
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 C20H26Cl2N2O4
MW 429.34
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.08

Activity Summary

Kd 5 meas. best 9.08
Ki 4 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1B adrenergic receptor
CHEMBL315
Kd 9.08 9.08 0.8 1
Alpha-1D adrenergic receptor
CHEMBL326
Kd 8.62 8.62 2.4 1
Alpha-1A adrenergic receptor
CHEMBL319
Kd 8.44 8.235 3.6 2
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.42 8.42 3.8 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.89 7.89 12.9 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.45 7.45 35.5 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.96 6.96 109.7 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 6.05 6.05 891.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23902232 10.1021/jm400867d Unchecked 4
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