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Assay Detail

CHEMBL1018991

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BHK
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.
Filosa R, Carmela Fulco M, Marinozzi M, Giacchè N, Macchiarulo A, Peduto A, Massa A, de Caprariis P, Thomsen C, Christoffersen CT, Pellicciari R.
Bioorg Med Chem (2009) 17 : 242 -250
PubMed 19042134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.24 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.24
CHEMBL467234 1 4.23
CHEMBL444718 1 -
CHEMBL450025 1 -
CHEMBL448885 1 -
CHEMBL445241 1 -
CHEMBL467235 1 -
CHEMBL33567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 570.0 nM 6.24
CHEMBL467234 Ki = 59000.0 nM 4.23
CHEMBL444718 Ki > 1000000.0 nM -
CHEMBL450025 Ki = 210000.0 nM -
CHEMBL448885 Ki > 1000000.0 nM -
CHEMBL445241 Ki > 300000.0 nM -
CHEMBL467235 Ki > 1000000.0 nM -
CHEMBL33567 Ki > 1000000.0 nM -