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Assay Detail

CHEMBL860565

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

Binding
Displacement of [3H]MPEP from mGluR5d in rat brain membrane
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 5 (CHEMBL2564)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.
Wållberg A, Nilsson K, Osterlund K, Peterson A, Elg S, Raboisson P, Bauer U, Hammerland LG, Mattsson JP.
Bioorg Med Chem Lett (2006) 16 : 1142 -1145
PubMed 16380255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.03 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202794 1 6.75
CHEMBL202845 1 6.50
CHEMBL239800 FENOBAM ANHYDROUS 2.0 1 6.34
CHEMBL202802 1 5.92
CHEMBL378365 1 5.89
CHEMBL203720 1 5.89
CHEMBL201827 1 5.80
CHEMBL380626 1 5.70
CHEMBL204445 1 5.47
CHEMBL204201 1 -
CHEMBL204289 1 -
CHEMBL201828 1 -
CHEMBL203713 1 -
CHEMBL380672 1 -
CHEMBL203566 1 -
CHEMBL377078 1 -
CHEMBL204115 1 -
CHEMBL204116 1 -
CHEMBL204202 1 -
CHEMBL382337 1 -
CHEMBL382681 1 -
CHEMBL275788 1 -
CHEMBL247495 1 -
CHEMBL424681 1 -
CHEMBL204799 1 -
CHEMBL204299 1 -
CHEMBL204392 1 -
CHEMBL381820 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202794 IC50 = 180.0 nM 6.75
CHEMBL202845 IC50 = 320.0 nM 6.50
CHEMBL239800 FENOBAM ANHYDROUS IC50 = 460.0 nM 6.34
CHEMBL202802 IC50 = 1200.0 nM 5.92
CHEMBL378365 IC50 = 1300.0 nM 5.89
CHEMBL203720 IC50 = 1300.0 nM 5.89
CHEMBL201827 IC50 = 1600.0 nM 5.80
CHEMBL380626 IC50 = 2000.0 nM 5.70
CHEMBL204445 IC50 = 3400.0 nM 5.47
CHEMBL204201 IC50 - -
CHEMBL204289 IC50 - -
CHEMBL201828 IC50 - -
CHEMBL203713 IC50 - -
CHEMBL380672 IC50 > 10000.0 nM -
CHEMBL203566 IC50 - -
CHEMBL377078 IC50 - -
CHEMBL204115 IC50 > 10000.0 nM -
CHEMBL204116 IC50 > 10000.0 nM -
CHEMBL204202 IC50 - -
CHEMBL382337 IC50 - -
CHEMBL382681 IC50 - -
CHEMBL275788 IC50 - -
CHEMBL247495 IC50 - -
CHEMBL424681 IC50 - -
CHEMBL204799 IC50 - -
CHEMBL204299 IC50 - -
CHEMBL204392 IC50 - -
CHEMBL381820 IC50 - -