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Compound Detail

CHEMBL3740374

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COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL3740374
Phase Preclinical
Structure Type MOL
InChI Key LBUNMGJPWDKBFD-PFEQFJNWSA-N
Parent Compound CHEMBL36622
Active Moiety CHEMBL36622
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

345.4
MW (Da)
2.51
ALogP
6
HBA
1
HBD
58.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25NO9
MW 435.43
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.20

Activity Summary

Ki 4 meas. best 7.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.98 7.98 10.5 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.95 7.95 11.2 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.39 7.39 40.7 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.14 7.14 72.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00484A Alpha-1D adrenergic receptor 1
- 10.1039/C4MD00484A Alpha-1B adrenergic receptor 1
- 10.1039/C4MD00484A Alpha-1A adrenergic receptor 1
- 10.1039/C4MD00484A 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine