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Compound Detail

CHEMBL3739613

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COc1ccc(C[C@@H]2CCCN2C(=O)c2ccccc2-c2nc(C)no2)cc1OC

Basic Information

ChEMBL ID CHEMBL3739613
Phase Preclinical
Structure Type MOL
InChI Key JZHKVYBNWKFHNL-KRWDZBQOSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

407.5
MW (Da)
3.91
ALogP
6
HBA
0
HBD
77.7
PSA (Ų)
0.62
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 C23H25N3O4
MW 407.47
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.24

Activity Summary

IC50 2 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
IC50 7.92 7.92 12.0 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 7.48 7.48 33.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 129.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C5MD00074B Liver microsome 1
- 10.1039/C5MD00074B Orexin/Hypocretin receptor type 1 1
- 10.1039/C5MD00074B Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine