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Compound Detail

CHEMBL454924

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COc1cc2c(cc1OC)C(CCc1ccc(F)c(F)c1)N(C(C(=O)NCC1CC1)c1ccccc1)CC2

Basic Information

ChEMBL ID CHEMBL454924
Phase Preclinical
Structure Type MOL
InChI Key MGTLLLVBSOYCAX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

520.6
MW (Da)
5.78
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.37
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 C31H34F2N2O3
MW 520.62
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.58

Activity Summary

IC50 2 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
IC50 7.85 7.85 14.0 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 6.26 6.26 552.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Orexin receptor type 2 IC50 = 14.0 nM 7.85 Inhibition of OX2 receptor 19199652
Orexin/Hypocretin receptor type 1 IC50 = 552.0 nM 6.26 Inhibition of OX1 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