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Compound Detail

CHEMBL1087455

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O=C1CCc2ccc(CC3CCN(C[C@@H]4COc5c(ccc6c5CC(=O)N6)O4)CC3)cc2N1

Basic Information

ChEMBL ID CHEMBL1087455
Phase Preclinical
Structure Type MOL
InChI Key VJQGVOVLQSAUIL-LJQANCHMSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
3.16
ALogP
5
HBA
2
HBD
79.9
PSA (Ų)
0.75
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29N3O4
MW 447.54
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.06

Activity Summary

Ki 3 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.72 8.72 1.9 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 8.7 8.7 2.0 1
D(2) dopamine receptor
CHEMBL217
Ki 8.1 8.1 8.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20347298 10.1016/j.bmcl.2010.02.105 D(2) dopamine receptor 2
20347298 10.1016/j.bmcl.2010.02.105 Adrenergic receptor alpha-1 1
20347298 10.1016/j.bmcl.2010.02.105 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine