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Compound Detail

CHEMBL4475736

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COC(=O)CN(C(C)=O)C(c1ccccc1)c1cc(Br)ccc1NC(=O)c1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL4475736
Phase Preclinical
Structure Type MOL
InChI Key GSPWQWXABHYRBK-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

529.8
MW (Da)
5.47
ALogP
4
HBA
1
HBD
75.7
PSA (Ų)
0.41
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H22BrClN2O4
MW 529.82
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.33

Activity Summary

IC50 2 meas. best 5.77
Ki 2 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
IC50 5.77 5.77 1700.0 1
Orexin receptor type 2
CHEMBL4792
Ki 5.6 5.6 2500.0 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
Ki 4.51 4.51 30700.0 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 4.27 4.27 53700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27546834 10.1021/acs.jmedchem.6b00333 Orexin receptor type 2 7
27546834 10.1021/acs.jmedchem.6b00333 Orexin/Hypocretin receptor type 1 7
27546834 10.1021/acs.jmedchem.6b00333 CHO 2
27546834 10.1021/acs.jmedchem.6b00333 Unchecked 1

Data from ChEMBL 36 via Core Engine