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Compound Detail

CHEMBL1956193

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CC(Oc1ccccc1C(F)(F)F)C1=NCCN1

Basic Information

ChEMBL ID CHEMBL1956193
Phase Preclinical
Structure Type MOL
InChI Key BFKLSSIIDDEGQB-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

258.2
MW (Da)
2.47
ALogP
3
HBA
1
HBD
33.6
PSA (Ų)
0.90
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H13F3N2O
MW 258.24
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness -0.67

Activity Summary

Ki 3 meas. best 6.74
EC50 2 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.74 6.74 182.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
EC50 6.62 6.62 239.9 1
Alpha-2C adrenergic receptor
CHEMBL1916
EC50 6.1 6.1 794.3 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.01 6.01 977.2 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 5.79 5.79 1621.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22341244 10.1016/j.bmc.2012.01.035 Alpha-2B adrenergic receptor 3
22341244 10.1016/j.bmc.2012.01.035 Alpha-2C adrenergic receptor 3
22341244 10.1016/j.bmc.2012.01.035 Alpha-2A adrenergic receptor 2

Data from ChEMBL 36 via Core Engine