eledoisin [Ligand Id: 2086] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL373569 (ELD 950, ELD-950, Eledoisin)
  • NK3 receptor/Neurokinin 3 receptor in Human [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
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  • NK1 receptor in Human [GtoPdb: 360] [UniProtKB: P25103]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
GtoPdb - - 6.6 pIC50 264.2 nM IC50 J Biol Chem (1996) 271: 20250-7 [PMID:8702757];
FEBS Lett (1992) 299: 90-5 [PMID:1312036]
ChEMBL Displacement of ([125I]-His3, MePhe7)-NKB from NK3R (unknown origin) transfected in CHO cells by gamma counting analysis B 7.02 pIC50 96 nM IC50 Bioorg Med Chem (2013) 21: 2413-2417 [PMID:23473945]
ChEMBL Activity at human NK3 receptor expressed in CHO cells assessed as increase in inositol phosphate generation F 8.18 pEC50 6.6 nM EC50 Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617]
ChEMBL Activity at human NK3 receptor assessed as stimulation of inositol phosphate generation in CHO cells F 8.24 pEC50 5.7 nM EC50 Bioorg Med Chem Lett (2006) 16: 5748-5751 [PMID:16950620]
ChEMBL Agonist activity at NK3R (unknown origin) transfected in CHO cells assessed as calcium influx at 10 mM F 9.66 pEC50 0.22 nM EC50 Bioorg Med Chem (2013) 21: 2413-2417 [PMID:23473945]
NK1 receptor in Human [GtoPdb: 360] [UniProtKB: P25103]
GtoPdb - - 8.6 pIC50 - - - J Biol Chem (1996) 271: 20250-7 [PMID:8702757]

ChEMBL data shown on this page come from version 32:

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]