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Compound Detail

CHEMBL4081842

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COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O

Basic Information

ChEMBL ID CHEMBL4081842
Phase Preclinical
Structure Type MOL
InChI Key PEXVMHLARUAHNC-MADCSZMMSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

364.2
MW (Da)
0.37
ALogP
8
HBA
5
HBD
193.4
PSA (Ų)
0.24
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H17N2O9P
MW 364.25
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness 0.34

Activity Summary

EC50 4 meas. best 6.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 4
CHEMBL2736
EC50 6.14 6.14 720.0 1
Metabotropic glutamate receptor 6
CHEMBL4573
EC50 5.96 5.96 1100.0 1
Metabotropic glutamate receptor 8
CHEMBL3228
EC50 4.75 4.75 18000.0 1
Metabotropic glutamate receptor 7
CHEMBL3777
EC50 4.2 4.2 63000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29397723 10.1021/acs.jmedchem.7b01438 Metabotropic glutamate receptor 6 1
29397723 10.1021/acs.jmedchem.7b01438 Metabotropic glutamate receptor 7 1
29397723 10.1021/acs.jmedchem.7b01438 Metabotropic glutamate receptor 4 1
29397723 10.1021/acs.jmedchem.7b01438 Metabotropic glutamate receptor 8 1
29397723 10.1021/acs.jmedchem.7b01438 Unchecked 1

Data from ChEMBL 36 via Core Engine