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Compound Detail

CHEMBL5203080

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COc1ccc(-c2cccc(C(=O)N(C)C)c2)cc1S(=O)(=O)Nc1ccc2c(c1)C(N(C)C(=O)Nc1ccccc1)CCC2

Basic Information

ChEMBL ID CHEMBL5203080
Phase Preclinical
Structure Type MOL
InChI Key JFMYCCJMEOAUMO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

612.8
MW (Da)
6.41
ALogP
5
HBA
2
HBD
108.0
PSA (Ų)
0.24
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H36N4O5S
MW 612.75
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -1.44

Activity Summary

EC50 2 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
EC50 6.85 6.85 140.0 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
EC50 5.49 5.49 3252.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35051577 10.1016/j.bmcl.2022.128555 Orexin/Hypocretin receptor type 1 2
35051577 10.1016/j.bmcl.2022.128555 Orexin receptor type 2 2
35051577 10.1016/j.bmcl.2022.128555 Unchecked 1

Data from ChEMBL 36 via Core Engine