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Compound Detail

CHEMBL122005

(S)-WILLARDIINE
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N[C@@H](Cn1ccc(=O)[nH]c1=O)C(=O)O

Basic Information

ChEMBL ID CHEMBL122005
Name (S)-WILLARDIINE
Phase Preclinical
Structure Type MOL
InChI Key FACUYWPMDKTVFU-BYPYZUCNSA-N
6
Targets
6
Activities
3
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

199.2
MW (Da)
-2.05
ALogP
5
HBA
3
HBD
118.2
PSA (Ų)
0.52
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C7H9N3O4
MW 199.17
Aromatic Rings 1
Heavy Atoms 14
NP-Likeness -0.02

Activity Summary

Ki 4 meas. best 6.41
EC50 1 meas. best 4.94
IC50 1 meas. best 4.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor 1
CHEMBL2009
Ki 6.41 6.41 386.0 1
Glutamate receptor 2
CHEMBL4016
Ki 6.05 6.05 898.0 1
Glutamate receptor 4
CHEMBL3190
Ki 5.05 5.05 8850.0 1
Glutamate receptor 1
CHEMBL3753
EC50 4.94 4.94 11500.0 1
Glutamate receptor ionotropic, kainate 5
CHEMBL2675
Ki 4.54 4.54 28900.0 1
Glutamate carboxypeptidase 2
CHEMBL1892
IC50 4.17 4.17 67000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9357531 10.1021/jm9702387 Glutamate receptor 1 1
9357531 10.1021/jm9702387 Glutamate receptor 2 1
9357531 10.1021/jm9702387 Glutamate receptor 4 1
9357531 10.1021/jm9702387 Glutamate receptor ionotropic, kainate 5 1
17567119 10.1021/jm070133w Glutamate carboxypeptidase 2 1
18811139 10.1021/jm800865a Glutamate receptor 1 1
18811139 10.1021/jm800865a Glutamate receptor 2 1
18811139 10.1021/jm800865a Glutamate receptor 3 1
17417631 10.1038/nchembio873 Unchecked 1

Data from ChEMBL 36 via Core Engine