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Compound Detail

CHEMBL63065

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COc1ccc(OCF)c(CN(C(C)=O)c2cc(F)ccc2Oc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL63065
Phase Preclinical
Structure Type MOL
InChI Key HNCYVWMTXRPXGY-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

413.4
MW (Da)
5.49
ALogP
4
HBA
0
HBD
48.0
PSA (Ų)
0.49
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21F2NO4
MW 413.42
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.93

Activity Summary

IC50 1 meas. best 8.77
Ki 1 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Translocator protein
CHEMBL4552
Ki 9.77 9.77 0.2 1
Translocator protein
CHEMBL4552
IC50 8.77 8.77 1.7 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.83 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15084121 10.1021/jm0304919 Mus musculus 6
15084121 10.1021/jm0304919 Translocator protein 1
15084121 10.1021/jm0304919 GABA-A receptor; anion channel 1
15084121 10.1021/jm0304919 No relevant target 1
15084121 10.1021/jm0304919 ADMET 1
12482423 10.1016/s0960-894x(02)00886-7 Translocator protein 1
12482423 10.1016/s0960-894x(02)00886-7 GABA-A receptor; anion channel 1
12482423 10.1016/s0960-894x(02)00886-7 No relevant target 1

Data from ChEMBL 36 via Core Engine