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Compound Detail

CHEMBL5192814

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COc1cccc(CC(=O)N(C)[C@H]2CCCc3ccc(NS(=O)(=O)c4cc(-c5cccc(C(=O)N(C)C)c5)ccc4OC)cc32)c1

Basic Information

ChEMBL ID CHEMBL5192814
Phase Preclinical
Structure Type MOL
InChI Key XONYJYAZEWRESR-YTTGMZPUSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

641.8
MW (Da)
5.95
ALogP
6
HBA
1
HBD
105.2
PSA (Ų)
0.23
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H39N3O6S
MW 641.79
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -1.31

Activity Summary

EC50 2 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
EC50 8.57 8.57 2.7 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
EC50 5.91 5.91 1244.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35051577 10.1016/j.bmcl.2022.128555 Orexin receptor type 2 2
35051577 10.1016/j.bmcl.2022.128555 Orexin/Hypocretin receptor type 1 1
35051577 10.1016/j.bmcl.2022.128555 Unchecked 1
37043436 10.1021/acs.jmedchem.2c01773 Mus musculus 1

Data from ChEMBL 36 via Core Engine