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Assay Detail

CHEMBL895144

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

Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
10
Total Activities
10
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 Intermediate

Target

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

Publication

Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.
Pellicciari R, Marinozzi M, Macchiarulo A, Fulco MC, Gafarova J, Serpi M, Giorgi G, Nielsen S, Thomsen C.
J Med Chem (2007) 50 : 4630 -4641
PubMed 17725337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 4.81 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.60
CHEMBL231157 1 4.47
CHEMBL389555 1 4.11
CHEMBL230951 1 4.06
CHEMBL389558 1 -
CHEMBL230950 1 -
CHEMBL389557 1 -
CHEMBL230949 1 -
CHEMBL389556 1 -
CHEMBL230852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 250.0 nM 6.60
CHEMBL231157 Ki = 34000.0 nM 4.47
CHEMBL389555 Ki = 77000.0 nM 4.11
CHEMBL230951 Ki = 87000.0 nM 4.06
CHEMBL389558 Ki > 300000.0 nM -
CHEMBL230950 Ki > 300000.0 nM -
CHEMBL389557 Ki > 300000.0 nM -
CHEMBL230949 Ki > 300000.0 nM -
CHEMBL389556 Ki > 300000.0 nM -
CHEMBL230852 Ki = 254000.0 nM -