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Compound Detail

CHEMBL344622

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COc1cc2c(cc1OC)CN(C(=O)[C@@H](NCc1cccs1)C(C)(C)C)CC2

Basic Information

ChEMBL ID CHEMBL344622
Phase Preclinical
Structure Type MOL
InChI Key RYPYLHGKDFBLIZ-HXUWFJFHSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

402.6
MW (Da)
3.85
ALogP
5
HBA
1
HBD
50.8
PSA (Ų)
0.80
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 C22H30N2O3S
MW 402.56
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.01

Activity Summary

IC50 4 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
IC50 7.6 7.6 25.0 2
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 5.95 5.95 1130.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14643355 10.1016/j.bmcl.2003.08.038 Orexin/Hypocretin receptor type 1 1
14643355 10.1016/j.bmcl.2003.08.038 Orexin receptor type 2 1
19199652 10.1021/jm801296d Orexin/Hypocretin receptor type 1 1
19199652 10.1021/jm801296d Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine