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Compound Detail

CHEMBL513351

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COc1ccc(C(C)C(F)(F)F)cc1CN[C@H]1CCCN[C@H]1c1ccccc1

Basic Information

ChEMBL ID CHEMBL513351
Phase Preclinical
Structure Type MOL
InChI Key PRVMNKWTNJEKFJ-XHRKEWCOSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

392.5
MW (Da)
4.94
ALogP
3
HBA
2
HBD
33.3
PSA (Ų)
0.73
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27F3N2O
MW 392.46
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.18

Activity Summary

Ki 2 meas. best 7.16
IC50 1 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.4 9.4 0.4 1
Cytochrome P450 2D6
CHEMBL289
Ki 7.16 7.16 70.0 1
Liver microsomes
CHEMBL613373
Ki 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18640044 10.1016/j.bmc.2008.06.047 Cytochrome P450 2D6 2
18640044 10.1016/j.bmc.2008.06.047 Mustela putorius furo 2
18640044 10.1016/j.bmc.2008.06.047 Liver microsomes 2
18640044 10.1016/j.bmc.2008.06.047 Substance-P receptor 1
18640044 10.1016/j.bmc.2008.06.047 Gerbillinae 1

Data from ChEMBL 36 via Core Engine