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Compound Detail

CHEMBL451281

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COc1cc2c(cc1OC)C(Cc1ccc(Oc3ncccn3)c(OC)c1)N(CC(=O)NCc1ccccc1)CC2

Basic Information

ChEMBL ID CHEMBL451281
Phase Preclinical
Structure Type MOL
InChI Key RRBYCHHICVPEJB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

554.6
MW (Da)
4.75
ALogP
8
HBA
1
HBD
95.0
PSA (Ų)
0.28
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34N4O5
MW 554.65
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.55

Activity Summary

IC50 2 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 7.28 7.28 52.0 1
Orexin receptor type 2
CHEMBL4792
IC50 6.62 6.62 240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Orexin/Hypocretin receptor type 1 IC50 = 52.0 nM 7.28 Inhibition of OX1 receptor 19199652
Orexin receptor type 2 IC50 = 240.0 nM 6.62 Inhibition of OX2 receptor 19199652

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

Data from ChEMBL 36 via Core Engine