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Compound Detail

CHEMBL142009

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COc1cc2c(cc1OC)CN(C(=O)[C@@H](NCc1ccncc1)C(C)(C)C)CC2

Basic Information

ChEMBL ID CHEMBL142009
Phase Preclinical
Structure Type MOL
InChI Key COFVZFLCAOUMJT-OAQYLSRUSA-N
1
Targets
4
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

397.5
MW (Da)
3.19
ALogP
5
HBA
1
HBD
63.7
PSA (Ų)
0.81
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H31N3O3
MW 397.52
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.57

Activity Summary

IC50 4 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
IC50 7.4 7.4 40.0 4

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19199652 10.1021/jm801296d Unchecked 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
14643355 10.1016/j.bmcl.2003.08.038 Orexin/Hypocretin receptor type 1 1
14643355 10.1016/j.bmcl.2003.08.038 Orexin receptor type 2 1
19199652 10.1021/jm801296d Orexin/Hypocretin receptor type 1 1
19199652 10.1021/jm801296d Orexin receptor type 2 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
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
38283232 10.1039/d3md00573a Orexin receptor type 2 1
38283232 10.1039/d3md00573a Orexin/Hypocretin receptor type 1 1

Data from ChEMBL 36 via Core Engine