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Compound Detail

CHEMBL3217244

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

Basic Information

ChEMBL ID CHEMBL3217244
Phase Preclinical
Structure Type MOL
InChI Key WNDMPEJJAWXNBF-QCUBGVIVSA-N
Parent Compound CHEMBL3039699
Active Moiety CHEMBL3039699
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
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

Ki 4 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.5 7.5 31.6 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.08 7.08 83.2 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.66 6.66 218.8 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.43 6.43 371.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine