(S)-VU0637120 [Ligand Id: 12608] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4780125
  • Y4 receptor/Neuropeptide Y receptor type 4 in Human [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Y4 receptor/Neuropeptide Y receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391]
ChEMBL Allosteric antagonist activity at eFYP-tagged human NPY4R expressed in COS7 cells co-expressing Gqi5-alpha assessed as inhibition of PP-induced Ca2+ flux by Fluo-2 AM dye based fluorescent assay relative to control F 5.4 pIC50 4000 nM IC50 J Med Chem (2021) 64: 2801-2814 [PMID:33595306]
ChEMBL Allosteric antagonist activity at eFYP-tagged human NPY4R expressed in COS7 cells co-expressing Gqi5-alpha assessed as inhibition of PP-induced Ca2+ flux by Fluo-2 AM dye based fluorescent assay relative to control F 5.4 pIC50 3981.07 nM IC50 J Med Chem (2021) 64: 2801-2814 [PMID:33595306]
GtoPdb Determined in vitro as modulator-induced decrease in Y4 receptor activation by pancreatic polypeptide - 5.57 pIC50 2700 nM IC50 J Med Chem (2021) 64: 2801-2814 [PMID:33595306]

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]