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Compound Detail

CHEMBL2385133

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[3H]c1ccc(CN(CC)C(=O)CN(c2ccc(OC([3H])([3H])[3H])nc2)S(=O)(=O)c2ccccc2C)cn1

Basic Information

ChEMBL ID CHEMBL2385133
Phase Preclinical
Structure Type MOL
InChI Key KJPHTXTWFHVJIG-MJVMYBOOSA-N
Parent Compound CHEMBL2385132
Active Moiety CHEMBL2385132
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

454.6
MW (Da)
3.04
ALogP
6
HBA
0
HBD
92.7
PSA (Ų)
0.49
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N4O4S
MW 462.58
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -2.18

Activity Summary

Ki 2 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
Ki 8.96 8.96 1.1 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
Ki 6.05 6.05 900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23601709 10.1016/j.bmcl.2013.03.079 Nucleic Acid 1
23891187 10.1016/j.bmcl.2013.06.057 Orexin receptor type 2 1
23891187 10.1016/j.bmcl.2013.06.057 Orexin/Hypocretin receptor type 1 1

Data from ChEMBL 36 via Core Engine