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Compound Detail

CHEMBL112351

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O=[N+]([O-])c1ccc2c(c1)CNC(C(F)(F)F)C2

Basic Information

ChEMBL ID CHEMBL112351
Phase Preclinical
Structure Type MOL
InChI Key AZEWYBRFBDWZGW-UHFFFAOYSA-N
3
Targets
8
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

246.2
MW (Da)
2.17
ALogP
3
HBA
1
HBD
55.2
PSA (Ų)
0.61
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H9F3N2O2
MW 246.19
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness -0.73

Activity Summary

Ki 8 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phenylethanolamine N-methyltransferase
CHEMBL2331
Ki 5.7 5.7 2000.0 1
Phenylethanolamine N-methyltransferase
CHEMBL4617
Ki 5.64 5.64 2300.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 5.47 5.47 3400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10091706 10.1016/s0960-894x(99)00022-0 Phenylethanolamine N-methyltransferase 1
10091706 10.1016/s0960-894x(99)00022-0 Adrenergic receptor alpha-2 1
10091706 10.1016/s0960-894x(99)00022-0 Unchecked 1
10464018 10.1021/jm980734a Phenylethanolamine N-methyltransferase 1
10464018 10.1021/jm980734a Adrenergic receptor alpha-2 1
10464018 10.1021/jm980734a Unchecked 1
15686930 10.1016/j.bmcl.2004.12.013 Adrenergic receptor alpha-2 1
15686930 10.1016/j.bmcl.2004.12.013 Alpha-2A adrenergic receptor 1
16169723 10.1016/j.bmcl.2005.08.033 Phenylethanolamine N-methyltransferase 1
16169723 10.1016/j.bmcl.2005.08.033 Adrenergic receptor alpha-2 1
16169723 10.1016/j.bmcl.2005.08.033 Unchecked 1

Data from ChEMBL 36 via Core Engine