VU0364770 [Ligand Id: 6234] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL556667 (N-(3-Chlorophenyl)Picolinamide)
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
ChEMBL Positive allosteric modulator activity at human mGlu4 receptor B 5.92 pEC50 1196 nM EC50 Bioorg Med Chem Lett (2015) 25: 3956-3960 [PMID:26231155]
ChEMBL Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization F 5.96 pEC50 1100 nM EC50 J Med Chem (2009) 52: 4115-4118 [PMID:19469556]
ChEMBL Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay F 5.96 pEC50 1100 nM EC50 Bioorg Med Chem Lett (2018) 28: 2641-2646 [PMID:29958762]
GtoPdb - - 6 pEC50 1100 nM EC50 J Pharmacol Exp Ther (2012) 340: 404-21 [PMID:22088953]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
ChEMBL Positive allosteric modulator activity at rat mGlu4 receptor B 6.48 pEC50 330 nM EC50 Bioorg Med Chem Lett (2015) 25: 3956-3960 [PMID:26231155]
GtoPdb - - 6.5 pEC50 290 nM EC50 J Pharmacol Exp Ther (2012) 340: 404-21 [PMID:22088953]
ChEMBL Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux B 6.54 pEC50 290 nM EC50 J Med Chem (2009) 52: 4115-4118 [PMID:19469556]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]