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Compound Detail

CHEMBL595840

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Cn1c(-c2ccccc2)cc2onc(-c3ccccc3)c2c1=O

Basic Information

ChEMBL ID CHEMBL595840
Phase Preclinical
Structure Type MOL
InChI Key LCNDUGHNYMJGIW-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

302.3
MW (Da)
3.86
ALogP
4
HBA
0
HBD
48.0
PSA (Ų)
0.56
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14N2O2
MW 302.33
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -0.70

Activity Summary

IC50 6 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 7
CHEMBL3879
IC50 7.7 7.7 20.0 1
Sentrin-specific protease 8
CHEMBL1741207
IC50 6.22 5.865 607.0 2
Sentrin-specific protease 7
CHEMBL1741213
IC50 5.94 5.94 1140.0 1
Sentrin-specific protease 6
CHEMBL1741215
IC50 5.82 5.82 1510.0 1
Caspase-3
CHEMBL2334
IC50 5.62 5.62 2400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Rattus norvegicus
CL - - Rattus norvegicus
F - % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20005101 10.1016/j.bmcl.2009.11.070 Rattus norvegicus 3
20005101 10.1016/j.bmcl.2009.11.070 Metabotropic glutamate receptor 7 1
20005101 10.1016/j.bmcl.2009.11.070 No relevant target 1
28655422 10.1016/j.bmcl.2017.06.039 dCTP pyrophosphatase 1 1

Data from ChEMBL 36 via Core Engine