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Compound Detail

CHEMBL4443478

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CCCCN(C)C(=O)N1CCC(=CC#Cc2cccc(C)n2)CC1

Basic Information

ChEMBL ID CHEMBL4443478
Phase Preclinical
Structure Type MOL
InChI Key DUDLUGRLTVPTNX-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

325.5
MW (Da)
3.62
ALogP
2
HBA
0
HBD
36.4
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27N3O
MW 325.46
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -0.98

Activity Summary

IC50 1 meas. best 4.87
Ki 1 meas. best 7.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 5
CHEMBL3227
Ki 7.69 7.69 20.4 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.87 4.87 13400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30624919 10.1021/acs.jmedchem.8b01226 Cytochrome P450 3A4 1
30624919 10.1021/acs.jmedchem.8b01226 Cytochrome P450 2D6 1
30624919 10.1021/acs.jmedchem.8b01226 Metabotropic glutamate receptor 1 1
30624919 10.1021/acs.jmedchem.8b01226 Metabotropic glutamate receptor 5 1

Data from ChEMBL 36 via Core Engine