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Compound Detail

CHEMBL3343258

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COc1ccc(OC[C@@]2(c3ccccc3)C[C@H]2C(=O)Nc2cc(C#N)ccn2)cc1OC

Basic Information

ChEMBL ID CHEMBL3343258
Phase Preclinical
Structure Type MOL
InChI Key PNEYBVJGZWJPGF-NBGIEHNGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

429.5
MW (Da)
3.95
ALogP
6
HBA
1
HBD
93.5
PSA (Ų)
0.58
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N3O4
MW 429.48
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.59

Activity Summary

Ki 2 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
Ki 7.47 7.47 34.0 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
Ki 6.99 6.99 103.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25267004 10.1016/j.bmc.2014.08.034 Orexin receptor type 2 1
25267004 10.1016/j.bmc.2014.08.034 Orexin/Hypocretin receptor type 1 1
25267004 10.1016/j.bmc.2014.08.034 ADMET 1
25267004 10.1016/j.bmc.2014.08.034 No relevant target 1

Data from ChEMBL 36 via Core Engine