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Assay Detail

CHEMBL4157622

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

Binding
Displacement of MPEP from mGluR5 (unknown origin) after 3 hrs by liquid scintillation counting method
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 5 (CHEMBL3227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isoxazolo[3,4-d]pyridazinones positively modulate the metabotropic glutamate subtypes 2 and 4.
Gates C, Backos DS, Reigan P, Kang HJ, Koerner C, Mirzaei J, Natale NR.
Bioorg Med Chem (2018) 26 : 4797 -4803
PubMed 30143366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.55 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239800 FENOBAM ANHYDROUS 2.0 2 7.50
CHEMBL4166199 1 5.72
CHEMBL4167825 1 5.51
CHEMBL4171187 1 -
CHEMBL4160584 1 -
CHEMBL4174628 1 -
CHEMBL4163974 1 -
CHEMBL4164391 1 -
CHEMBL4172276 1 -
CHEMBL4175689 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239800 FENOBAM ANHYDROUS Ki = 31.62 nM 7.50
CHEMBL239800 FENOBAM ANHYDROUS Ki = 33.0 nM 7.48
CHEMBL4166199 Ki = 1883.0 nM 5.72
CHEMBL4167825 Ki = 3077.0 nM 5.51
CHEMBL4171187 Ki > 10000.0 nM -
CHEMBL4160584 Ki > 10000.0 nM -
CHEMBL4174628 Ki > 10000.0 nM -
CHEMBL4163974 Ki > 10000.0 nM -
CHEMBL4164391 Ki > 10000.0 nM -
CHEMBL4172276 Ki > 10000.0 nM -
CHEMBL4175689 Ki - -