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Compound Detail

CHEMBL489485

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COc1cc2c(cc1OC)C(Cc1ccc(Cl)c(Cl)c1)N(CC(=O)NCc1ccccc1)CC2

Basic Information

ChEMBL ID CHEMBL489485
Phase Preclinical
Structure Type MOL
InChI Key FIPKTJXYARUTNO-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

499.4
MW (Da)
5.47
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.45
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 C27H28Cl2N2O3
MW 499.44
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.58

Activity Summary

IC50 4 meas. best 6.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 6.93 6.93 118.0 2
Orexin receptor type 2
CHEMBL4792
IC50 6.55 6.55 281.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19199652 10.1021/jm801296d Orexin/Hypocretin receptor type 1 1
19199652 10.1021/jm801296d Orexin receptor type 2 1
26317591 10.1021/acs.jmedchem.5b00832 Orexin receptor type 2 1
26317591 10.1021/acs.jmedchem.5b00832 Orexin/Hypocretin receptor type 1 1

Data from ChEMBL 36 via Core Engine