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Assay Detail

CHEMBL888663

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

Functional
Antagonist activity at human mGluR5 receptor expressed in CHOK1 cells assessed as inhibition of glutamate-mediated internal calcium mobilization
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Carroll FI, Kotturi SV, Navarro HA, Mascarella SW, Gilmour BP, Smith FL, Gabra BH, Dewey WL.
J Med Chem (2007) 50 : 3388 -3391
PubMed 17569516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.13 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66654 1 8.82
CHEMBL227200 1 8.64
CHEMBL390802 1 8.38
CHEMBL390803 1 8.22
CHEMBL390805 1 7.28
CHEMBL387873 1 7.10
CHEMBL227202 1 7.07
CHEMBL227201 1 7.02
CHEMBL226832 1 6.88
CHEMBL227199 1 6.85
CHEMBL390804 1 6.51
CHEMBL226831 1 6.29
CHEMBL226833 1 5.72
CHEMBL227157 1 5.05
CHEMBL229707 1 -
CHEMBL390494 1 -
CHEMBL441719 1 -
CHEMBL375680 1 -
CHEMBL227156 1 -
CHEMBL226834 1 -
CHEMBL226621 1 -
CHEMBL226830 1 -
CHEMBL226783 1 -
CHEMBL390801 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66654 IC50 = 1.5 nM 8.82
CHEMBL227200 IC50 = 2.3 nM 8.64
CHEMBL390802 IC50 = 4.2 nM 8.38
CHEMBL390803 IC50 = 6.0 nM 8.22
CHEMBL390805 IC50 = 52.0 nM 7.28
CHEMBL387873 IC50 = 80.0 nM 7.10
CHEMBL227202 IC50 = 85.0 nM 7.07
CHEMBL227201 IC50 = 96.0 nM 7.02
CHEMBL226832 IC50 = 132.0 nM 6.88
CHEMBL227199 IC50 = 140.0 nM 6.85
CHEMBL390804 IC50 = 312.0 nM 6.51
CHEMBL226831 IC50 = 510.0 nM 6.29
CHEMBL226833 IC50 = 1890.0 nM 5.72
CHEMBL227157 IC50 = 8900.0 nM 5.05
CHEMBL229707 IC50 - -
CHEMBL390494 IC50 - -
CHEMBL441719 IC50 - -
CHEMBL375680 IC50 - -
CHEMBL227156 IC50 - -
CHEMBL226834 IC50 - -
CHEMBL226621 IC50 - -
CHEMBL226830 IC50 - -
CHEMBL226783 IC50 - -
CHEMBL390801 IC50 - -