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Compound Detail

CHEMBL1095413

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O=C1/C(=C\c2cccnc2)C(c2ccc(OC(F)(F)F)cc2)n2cccc21

Basic Information

ChEMBL ID CHEMBL1095413
Phase Preclinical
Structure Type MOL
InChI Key NUADOLYUKJMRKY-WJDWOHSUSA-N

Known Names

MR-16089
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
1
Known Names

Molecular Properties

370.3
MW (Da)
4.65
ALogP
4
HBA
0
HBD
44.1
PSA (Ų)
0.63
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 C20H13F3N2O2
MW 370.33
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.83

Activity Summary

IC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 7.4 6.6 40.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aromatase IC50 = 40.0 nM 7.4 Inhibition of human placental microsome CYP19 20413308
Aromatase IC50 = 1600.0 nM 5.8 Inhibition of aromatase (unknown origin) 24331756

Literature References

PubMed DOI Target Context # Activities
20413308 10.1016/j.bmcl.2010.03.113 Aromatase 1
24331756 10.1016/j.bmc.2013.11.040 Aromatase 1

Data from ChEMBL 36 via Core Engine