SR48527 [Ligand Id: 1581] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL461604 (SR-48527)
  • NTS2 receptor/Neurotensin receptor 2 in Rat [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384]
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  • NTS1 receptor in Rat [GtoPdb: 309] [UniProtKB: P20789]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NTS2 receptor/Neurotensin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384]
ChEMBL Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting B 6.19 pKi 644 nM Ki J Med Chem (2014) 57: 5318-5332 [PMID:24856674]
ChEMBL Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay F 6.66 pEC50 217 nM EC50 J Med Chem (2014) 57: 5318-5332 [PMID:24856674]
NTS1 receptor in Rat [GtoPdb: 309] [UniProtKB: P20789]
GtoPdb - - 7.5 pKi - - - Mol Pharmacol (1995) 47: 1050-6 [PMID:7746272]

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]