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Compound Detail

CHEMBL1645547

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Cc1nccc2c1[nH]c1cc(OCCCC(F)(F)F)ccc12

Basic Information

ChEMBL ID CHEMBL1645547
Phase Preclinical
Structure Type MOL
InChI Key DTZUQYMIOUZBFU-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

308.3
MW (Da)
4.75
ALogP
2
HBA
1
HBD
37.9
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15F3N2O
MW 308.30
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.33

Activity Summary

IC50 2 meas. best 8.3
Ki 1 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] A
CHEMBL1951
Ki 8.44 8.44 3.6 1
Amine oxidase [flavin-containing] A
CHEMBL1951
IC50 8.3 8.3 5.0 1
T98G
CHEMBL614775
IC50 4.07 4.07 86000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22770529 10.1021/jm300542e NON-PROTEIN TARGET 2
21183355 10.1016/j.bmc.2010.11.041 Amine oxidase [flavin-containing] A 1
21183355 10.1016/j.bmc.2010.11.041 Amine oxidase [flavin-containing] B 1
22770529 10.1021/jm300542e OE33 1
22770529 10.1021/jm300542e Hs 683 1
22770529 10.1021/jm300542e T98G 1
25747498 10.1016/j.ejmech.2015.02.044 Hs 683 1
33528252 10.1021/acs.jmedchem.0c01887 Amine oxidase [flavin-containing] A 1

Data from ChEMBL 36 via Core Engine