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Assay Detail

CHEMBL898095

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

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

Assay Information

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

Target

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

Publication

Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Milbank JB, Knauer CS, Augelli-Szafran CE, Sakkab-Tan AT, Lin KK, Yamagata K, Hoffman JK, Zhuang N, Thomas J, Galatsis P, Wendt JA, Mickelson JW, Schwarz RD, Kinsora JJ, Lotarski SM, Stakich K, Gillespie KK, Lam WW, Mutlib AE.
Bioorg Med Chem Lett (2007) 17 : 4415 -4418
PubMed 17590335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.68 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66654 1 8.24
CHEMBL232188 1 7.66
CHEMBL244796 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66654 Ki = 5.7 nM 8.24
CHEMBL232188 Ki = 22.0 nM 7.66
CHEMBL244796 Ki = 72.0 nM 7.14