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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]