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Compound Detail

CHEMBL444407

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COc1ccc(CC2c3cc(OC)c(OC)cc3CCN2C(C(=O)Nc2ccc3c(c2)OCO3)c2ccccc2)cc1OC

Basic Information

ChEMBL ID CHEMBL444407
Phase Preclinical
Structure Type MOL
InChI Key XLAYTQSXXHBEQX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

596.7
MW (Da)
5.97
ALogP
8
HBA
1
HBD
87.7
PSA (Ų)
0.24
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H36N2O7
MW 596.68
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -0.25

Activity Summary

IC50 2 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 7.68 7.68 21.0 1
Orexin receptor type 2
CHEMBL4792
IC50 5.74 5.74 1814.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Orexin/Hypocretin receptor type 1 IC50 = 21.0 nM 7.68 Inhibition of OX1 receptor 19199652
Orexin receptor type 2 IC50 = 1814.0 nM 5.74 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