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Compound Detail

CHEMBL2112974

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COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H]1CN2

Basic Information

ChEMBL ID CHEMBL2112974
Phase Preclinical
Structure Type MOL
InChI Key DPWMWVBVQVDTJY-CVDCTZTESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

457.0
MW (Da)
3.32
ALogP
7
HBA
1
HBD
58.6
PSA (Ų)
0.72
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29ClN4O3
MW 456.97
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.52

Activity Summary

Ki 2 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.64 7.64 23.0 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.82 6.82 151.0 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