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Compound Detail

CHEMBL4590911

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

Basic Information

ChEMBL ID CHEMBL4590911
Phase Preclinical
Structure Type MOL
InChI Key HEWBJUZWTAYGRE-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

282.4
MW (Da)
3.09
ALogP
2
HBA
0
HBD
33.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H22N2O
MW 282.39
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness -0.80

Activity Summary

IC50 1 meas. best 5.21
Ki 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 5
CHEMBL3227
Ki 7.62 7.62 24.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 5.21 5.21 6100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30624919 10.1021/acs.jmedchem.8b01226 ADMET 2
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 Cytochrome P450 1A2 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