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Compound Detail

CHEMBL131155

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COc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C(C)=O)CC1

Basic Information

ChEMBL ID CHEMBL131155
Phase Preclinical
Structure Type MOL
InChI Key LDENPNCRFIDJLK-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
3.63
ALogP
3
HBA
0
HBD
42.4
PSA (Ų)
0.79
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N2O2
MW 348.45
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.36

Activity Summary

IC50 2 meas. best 5.47
Ki 1 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL4701
Ki 5.8 5.8 1600.0 1
Platelet-activating factor receptor
CHEMBL250
IC50 5.47 5.47 3400.0 1
Protein farnesyltransferase
CHEMBL2094108
IC50 4.25 4.25 56000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1671420 10.1021/jm00105a069 Platelet-activating factor receptor 2
1671420 10.1021/jm00105a069 Histamine H1 receptor 1
9406600 10.1021/jm970291v Protein farnesyltransferase 1

Data from ChEMBL 36 via Core Engine