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Compound Detail

CHEMBL2112981

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C(=C/c1ccccc1)\CN1CCN(C[C@@H]2ON=C3c4ccccc4NC[C@H]32)CC1

Basic Information

ChEMBL ID CHEMBL2112981
Phase Preclinical
Structure Type MOL
InChI Key HCMWMLSNHRNVSJ-BASMTRSQSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

388.5
MW (Da)
3.16
ALogP
5
HBA
1
HBD
40.1
PSA (Ų)
0.85
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O
MW 388.51
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.31

Activity Summary

Ki 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.82 7.82 15.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 7.7 7.7 20.0 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 7.08 7.08 84.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15771448 10.1021/jm049619s Alpha-2A adrenergic receptor 1
15771448 10.1021/jm049619s Alpha-2C adrenergic receptor 1
15771448 10.1021/jm049619s Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine