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Compound Detail

CHEMBL4741048

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COc1ccc([C@H]2CCCN2C(=O)c2ccc(OCc3cn4ccccc4n3)cc2)c(OC)c1

Basic Information

ChEMBL ID CHEMBL4741048
Phase Preclinical
Structure Type MOL
InChI Key FZAISNFIIYVWPY-XMMPIXPASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
4.91
ALogP
6
HBA
0
HBD
65.3
PSA (Ų)
0.39
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27N3O4
MW 457.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.56

Activity Summary

Ki 2 meas. best 4.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
Ki 4.68 4.68 20893.0 1
Unchecked
CHEMBL612545
Ki 4.48 4.48 33113.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32977721 10.1021/acs.jmedchem.0c00964 Orexin/Hypocretin receptor type 1 1
32977721 10.1021/acs.jmedchem.0c00964 Unchecked 1
32977721 10.1021/acs.jmedchem.0c00964 Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine