Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1032407

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

Functional
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 1 (CHEMBL2892)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Ito S, Satoh A, Nagatomi Y, Hirata Y, Suzuki G, Kimura T, Satow A, Maehara S, Hikichi H, Hata M, Kawamoto H, Ohta H.
Bioorg Med Chem (2008) 16 : 9817 -9829
PubMed 18849168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.30 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL456823 1 8.82
CHEMBL502882 1 8.51
CHEMBL456196 1 8.48
CHEMBL452618 1 7.92
CHEMBL461673 1 7.80
CHEMBL511355 1 7.62
CHEMBL460827 1 7.51
CHEMBL460391 1 7.41
CHEMBL511352 1 7.24
CHEMBL457872 1 6.82
CHEMBL461035 1 6.80
CHEMBL453249 1 6.75
CHEMBL457026 1 6.75
CHEMBL461034 1 6.54
CHEMBL457873 1 6.00
CHEMBL461033 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL456823 IC50 = 1.5 nM 8.82
CHEMBL502882 IC50 = 3.1 nM 8.51
CHEMBL456196 IC50 = 3.3 nM 8.48
CHEMBL452618 IC50 = 12.0 nM 7.92
CHEMBL461673 IC50 = 16.0 nM 7.80
CHEMBL511355 IC50 = 24.0 nM 7.62
CHEMBL460827 IC50 = 31.0 nM 7.51
CHEMBL460391 IC50 = 39.0 nM 7.41
CHEMBL511352 IC50 = 58.0 nM 7.24
CHEMBL457872 IC50 = 150.0 nM 6.82
CHEMBL461035 IC50 = 160.0 nM 6.80
CHEMBL453249 IC50 = 180.0 nM 6.75
CHEMBL457026 IC50 = 180.0 nM 6.75
CHEMBL461034 IC50 = 290.0 nM 6.54
CHEMBL457873 IC50 = 1000.0 nM 6.00
CHEMBL461033 IC50 = 1600.0 nM 5.80