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Compound Detail

CHEMBL3742301

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Cc1cccc(-c2sc(C)nc2C(=O)N2CCC[C@H]2Cc2ccc3c(c2)OCCO3)c1

Basic Information

ChEMBL ID CHEMBL3742301
Phase Preclinical
Structure Type MOL
InChI Key YXOSYZGHPNXTKL-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

434.6
MW (Da)
5.05
ALogP
5
HBA
0
HBD
51.7
PSA (Ų)
0.58
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26N2O3S
MW 434.56
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.22

Activity Summary

IC50 2 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 7.46 7.46 35.0 1
Orexin receptor type 2
CHEMBL4792
IC50 7.41 7.41 39.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1040.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C5MD00074B Liver microsome 1
- 10.1039/C5MD00074B Orexin/Hypocretin receptor type 1 1
- 10.1039/C5MD00074B Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine