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Assay Detail

CHEMBL1115329

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Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 4 (CHEMBL2787)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
Selvam C, Oueslati N, Lemasson IA, Brabet I, Rigault D, Courtiol T, Cesarini S, Triballeau N, Bertrand HO, Goudet C, Pin JP, Acher FC.
J Med Chem (2010) 53 : 2797 -2813
PubMed 20218620 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.53 6.89
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33567 1 6.89
CHEMBL1092243 1 6.00
CHEMBL1076865 1 6.00
CHEMBL1092315 1 5.62
CHEMBL1089515 1 5.21
CHEMBL1092316 1 5.14
CHEMBL1089852 1 5.13
CHEMBL1093009 1 5.07
CHEMBL1093612 1 4.70
CHEMBL1092312 1 -
CHEMBL1092314 1 -
CHEMBL1089174 1 -
CHEMBL1089175 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33567 EC50 = 130.0 nM 6.89
CHEMBL1092243 EC50 = 1000.0 nM 6.00
CHEMBL1076865 EC50 = 1000.0 nM 6.00
CHEMBL1092315 EC50 = 2400.0 nM 5.62
CHEMBL1089515 EC50 = 6150.0 nM 5.21
CHEMBL1092316 EC50 = 7200.0 nM 5.14
CHEMBL1089852 EC50 = 7400.0 nM 5.13
CHEMBL1093009 EC50 = 8500.0 nM 5.07
CHEMBL1093612 EC50 = 20000.0 nM 4.70
CHEMBL1092312 EC50 = 141000.0 nM -
CHEMBL1092314 EC50 = 123000.0 nM -
CHEMBL1089174 EC50 = 209000.0 nM -
CHEMBL1089175 Activity - -