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Compound Detail

CHEMBL2112969

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COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(CCOc4ccc(F)cc4)CC3)[C@@H]1CN2

Basic Information

ChEMBL ID CHEMBL2112969
Phase Preclinical
Structure Type MOL
InChI Key AIWNTZODSQLIEU-RDPSFJRHSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

470.6
MW (Da)
2.68
ALogP
8
HBA
1
HBD
67.8
PSA (Ų)
0.64
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 C25H31FN4O4
MW 470.55
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.64

Activity Summary

Ki 3 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 8.8 8.8 1.6 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 8.04 8.04 9.1 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.81 6.81 154.0 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