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Assay Detail

CHEMBL864285

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

Functional
Activity at human mGluR5 assessed as effect on glutamate-induced calcium ion mobilization by FLIPR
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Bach P, Nilsson K, Wållberg A, Bauer U, Hammerland LG, Peterson A, Svensson T, Osterlund K, Karis D, Boije M, Wensbo D.
Bioorg Med Chem Lett (2006) 16 : 4792 -4795
PubMed 16839764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.59 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214640 1 7.82
CHEMBL66654 1 7.66
CHEMBL215941 1 7.44
CHEMBL292065 1 7.11
CHEMBL215957 1 7.08
CHEMBL378219 1 7.00
CHEMBL212129 1 6.99
CHEMBL212130 1 6.94
CHEMBL1161889 1 6.52
CHEMBL213102 1 6.40
CHEMBL215282 1 6.38
CHEMBL215861 1 6.34
CHEMBL215561 1 6.08
CHEMBL215702 1 5.83
CHEMBL212018 1 5.81
CHEMBL215120 1 5.60
CHEMBL384991 1 5.10
CHEMBL215300 1 -
CHEMBL213220 1 -
CHEMBL215058 1 -
CHEMBL215149 1 -
CHEMBL215098 1 -
CHEMBL215097 1 -
CHEMBL214094 1 -
CHEMBL213985 1 -
CHEMBL214538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214640 IC50 = 15.0 nM 7.82
CHEMBL66654 IC50 = 22.0 nM 7.66
CHEMBL215941 IC50 = 36.0 nM 7.44
CHEMBL292065 IC50 = 77.0 nM 7.11
CHEMBL215957 IC50 = 83.0 nM 7.08
CHEMBL378219 IC50 = 101.0 nM 7.00
CHEMBL212129 IC50 = 102.0 nM 6.99
CHEMBL212130 IC50 = 115.0 nM 6.94
CHEMBL1161889 IC50 = 300.0 nM 6.52
CHEMBL213102 IC50 = 397.0 nM 6.40
CHEMBL215282 IC50 = 416.0 nM 6.38
CHEMBL215861 IC50 = 455.0 nM 6.34
CHEMBL215561 IC50 = 825.0 nM 6.08
CHEMBL215702 IC50 = 1490.0 nM 5.83
CHEMBL212018 IC50 = 1540.0 nM 5.81
CHEMBL215120 IC50 = 2490.0 nM 5.60
CHEMBL384991 IC50 = 7926.0 nM 5.10
CHEMBL215300 IC50 > 10000.0 nM -
CHEMBL213220 IC50 > 10000.0 nM -
CHEMBL215058 IC50 > 3000.0 nM -
CHEMBL215149 IC50 > 10000.0 nM -
CHEMBL215098 IC50 > 10000.0 nM -
CHEMBL215097 IC50 > 10000.0 nM -
CHEMBL214094 IC50 > 10000.0 nM -
CHEMBL213985 IC50 > 10000.0 nM -
CHEMBL214538 IC50 > 10000.0 nM -