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Assay Detail

CHEMBL710045

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Functional
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 1 (CHEMBL3772)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chiral resolution, pharmacological characterization, and receptor docking of the noncompetitive mGlu1 receptor antagonist (+/-)-2-hydroxyimino- 1a, 2-dihydro-1H-7-oxacyclopropa[b]naphthalene-7a-carboxylic acid ethyl ester.
Ott D, Floersheim P, Inderbitzin W, Stoehr N, Francotte E, Lecis G, Richert P, Rihs G, Flor PJ, Kuhn R, Gasparini F.
J Med Chem (2000) 43 : 4428 -4436
PubMed 11087567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.89 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2111944 1 6.37
CHEMBL138082 1 5.92
CHEMBL434064 1 5.85
CHEMBL2111945 1 5.82
CHEMBL327783 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2111944 IC50 = 430.0 nM 6.37
CHEMBL138082 IC50 = 1200.0 nM 5.92
CHEMBL434064 IC50 = 1400.0 nM 5.85
CHEMBL2111945 IC50 = 1500.0 nM 5.82
CHEMBL327783 IC50 = 3400.0 nM 5.47