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Compound Detail

CHEMBL220629

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COc1ccnc(-c2cnc(C(=O)CCCCCCc3ccccc3)o2)c1

Basic Information

ChEMBL ID CHEMBL220629
Phase Preclinical
Structure Type MOL
InChI Key APJNZPUSSLCYBE-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

364.4
MW (Da)
5.12
ALogP
5
HBA
0
HBD
65.2
PSA (Ų)
0.37
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N2O3
MW 364.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.33

Activity Summary

IC50 2 meas. best 8.77
Ki 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fatty-acid amide hydrolase 1
CHEMBL2243
Ki 9.1 9.1 0.8 1
Fatty-acid amide hydrolase 1
CHEMBL3229
Ki 9.1 9.1 0.8 1
Fatty-acid amide hydrolase 1
CHEMBL2243
IC50 8.77 8.77 1.7 1
Liver carboxylesterase 1
CHEMBL2265
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17279740 10.1021/jm0611509 Fatty-acid amide hydrolase 1 2
17279740 10.1021/jm0611509 Unchecked 2
17279740 10.1021/jm0611509 Neutral cholesterol ester hydrolase 1 1
17279740 10.1021/jm0611509 Liver carboxylesterase 1 1
18053726 10.1016/j.bmc.2007.11.015 Fatty-acid amide hydrolase 1 1

Data from ChEMBL 36 via Core Engine