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Assay Detail

CHEMBL885955

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

Binding
Displacement of [3H]MPEP from mGlu5 receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
Jaeschke G, Porter R, Büttelmann B, Ceccarelli SM, Guba W, Kuhn B, Kolczewski S, Huwyler J, Mutel V, Peters JU, Ballard T, Prinssen E, Vieira E, Wichmann J, Spooren W.
Bioorg Med Chem Lett (2007) 17 : 1307 -1311
PubMed 17196387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.88 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245404 1 8.52
CHEMBL66654 1 8.40
CHEMBL415083 1 8.30
CHEMBL245406 1 8.00
CHEMBL394923 1 7.58
CHEMBL245405 1 7.41
CHEMBL239800 FENOBAM ANHYDROUS 2.0 1 7.21
CHEMBL391604 1 7.11
CHEMBL245606 1 6.78
CHEMBL394922 1 6.54
CHEMBL381820 1 6.50
CHEMBL391401 1 6.23
CHEMBL245607 1 6.18
CHEMBL246235 1 6.16
CHEMBL245403 1 5.95
CHEMBL247495 1 5.87
CHEMBL239799 1 5.60
CHEMBL246234 1 5.57
CHEMBL239802 1 -
CHEMBL239801 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245404 IC50 = 3.0 nM 8.52
CHEMBL66654 IC50 = 4.0 nM 8.40
CHEMBL415083 IC50 = 5.0 nM 8.30
CHEMBL245406 IC50 = 10.0 nM 8.00
CHEMBL394923 IC50 = 26.0 nM 7.58
CHEMBL245405 IC50 = 39.0 nM 7.41
CHEMBL239800 FENOBAM ANHYDROUS IC50 = 61.0 nM 7.21
CHEMBL391604 IC50 = 78.0 nM 7.11
CHEMBL245606 IC50 = 166.0 nM 6.78
CHEMBL394922 IC50 = 286.0 nM 6.54
CHEMBL381820 IC50 = 320.0 nM 6.50
CHEMBL391401 IC50 = 587.0 nM 6.23
CHEMBL245607 IC50 = 663.0 nM 6.18
CHEMBL246235 IC50 = 700.0 nM 6.16
CHEMBL245403 IC50 = 1120.0 nM 5.95
CHEMBL247495 IC50 = 1360.0 nM 5.87
CHEMBL239799 IC50 = 2520.0 nM 5.60
CHEMBL246234 IC50 = 2670.0 nM 5.57
CHEMBL239802 IC50 > 5000.0 nM -
CHEMBL239801 IC50 > 5000.0 nM -