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Compound Detail

CHEMBL452001

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CN(C)c1ccc(/C=C2\COc3ccccc3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL452001
Phase Preclinical
Structure Type MOL
InChI Key LNRGWJPLWJSMSG-SDNWHVSQSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

279.3
MW (Da)
3.41
ALogP
3
HBA
0
HBD
29.5
PSA (Ų)
0.79
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17NO2
MW 279.34
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.37

Activity Summary

IC50 4 meas. best 8.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 8.07 6.57 8.5 2
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.92 4.92 12000.0 1
L1210
CHEMBL386
IC50 4.04 4.04 91000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17692998 10.1016/j.ejmech.2007.06.017 ADMET 3
17692998 10.1016/j.ejmech.2007.06.017 CCRF-CEM 2
24169316 10.1016/j.bmc.2013.10.004 Amine oxidase [flavin-containing] B 2
17692998 10.1016/j.ejmech.2007.06.017 NON-PROTEIN TARGET 1
17692998 10.1016/j.ejmech.2007.06.017 L1210 1
17692998 10.1016/j.ejmech.2007.06.017 HSC-2 1
17692998 10.1016/j.ejmech.2007.06.017 HSC-3 1
17692998 10.1016/j.ejmech.2007.06.017 HSC-4 1
17692998 10.1016/j.ejmech.2007.06.017 HL-60 1
17692998 10.1016/j.ejmech.2007.06.017 Mus musculus 1
21405131 10.1021/jm1013709 Amine oxidase [flavin-containing] A 1
21405131 10.1021/jm1013709 Amine oxidase [flavin-containing] B 1
- 10.1007/s00044-012-0058-2 Estrogen receptor 1
- 10.1007/s00044-012-0058-2 MVLN 1

Data from ChEMBL 36 via Core Engine