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Compound Detail

CHEMBL599726

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COc1ccc(C(O)(c2ccc(OC)c(OC)c2)C2CCN(C(=O)Oc3ccc([N+](=O)[O-])cc3)CC2)cc1OC

Basic Information

ChEMBL ID CHEMBL599726
Phase Preclinical
Structure Type MOL
InChI Key MVYBTKBQHTXWBA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

552.6
MW (Da)
4.78
ALogP
9
HBA
1
HBD
129.8
PSA (Ų)
0.29
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32N2O9
MW 552.58
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.59

Activity Summary

IC50 2 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Monoglyceride lipase
CHEMBL5774
IC50 5.89 5.89 1300.0 1
Monoacylglycerol lipase ABHD6
CHEMBL5010
IC50 5.16 5.16 6960.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Monoglyceride lipase IC50 = 1300.0 nM 5.89 Inhibition of MAGL in mouse brain membrane 20099888
Monoacylglycerol lipase ABHD6 IC50 = 6960.0 nM 5.16 Inhibition of ABHD6 in mouse brain membrane 20099888

Literature References

PubMed DOI Target Context # Activities
20099888 10.1021/jm9016976 Fatty-acid amide hydrolase 1 1
20099888 10.1021/jm9016976 Monoglyceride lipase 1
20099888 10.1021/jm9016976 Monoacylglycerol lipase ABHD6 1
20099888 10.1021/jm9016976 Unchecked 1

Data from ChEMBL 36 via Core Engine