RP67580 [Ligand Id: 3522] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL131171 (RP-67580)
  • NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
  • NK1 receptor/Neurokinin 1 receptor in Mouse [ChEMBL: CHEMBL2668] [GtoPdb: 360] [UniProtKB: P30548]
  • NK1 receptor/Neurokinin 1 receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
  • Neurokinin 1 receptor in Guinea pig [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL Compound was tested for its binding affinity to NK1 receptor in [3H]SP binding assay on human IM9 lymphoblasts cultured cell line. B 7.31 pIC50 49 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1591-1594
ChEMBL Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1996) 39: 736-748 [PMID:8576917]
GtoPdb - - 7.7 pIC50 - - Ki J Biol Chem (1992) 267: 25668-71 [PMID:1281470]
NK1 receptor/Neurokinin 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2668] [GtoPdb: 360] [UniProtKB: P30548]
ChEMBL Inhibitory activity against Tachykinin receptor 1 in mouse brain using [125I]-labeled Boltan-Hunter substance P as radioligand B 8.06 pIC50 8.7 nM IC50 J. Med. Chem. (1996) 39: 736-748 [PMID:8576917]
NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
ChEMBL Tested for binding affinity towards Tachykinin receptor 1 by using [3H]SP binding assay in rat brain membranes B 8.38 pKi 4.16 nM Ki Bioorg. Med. Chem. Lett. (1992) 2: 37-40
ChEMBL Inhibition of [3H]SP binding in rat brain membranes B 5.38 pIC50 4160 nM IC50 J. Med. Chem. (1995) 38: 4793-4805 [PMID:7490729]
ChEMBL Compound was tested for its binding affinity to NK1 receptor in [3H]SP binding assay on rat brain membranes. B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1591-1594
ChEMBL Inhibitory activity against Tachykinin receptor 1 in rat brain using [125I]-labeled Boltan-Hunter substance P as radioligand B 8.17 pIC50 6.7 nM IC50 J. Med. Chem. (1996) 39: 736-748 [PMID:8576917]
Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
ChEMBL Tested for inhibition of contractile effects of Tachykinin receptor 1 in guinea pig ileum preparation. F 7.2 pKd 63.1 nM Kd Bioorg. Med. Chem. Lett. (1992) 2: 37-40
ChEMBL Inhibitory activity against Tachykinin receptor 1 in guinea pig brain using [125I]-labeled Boltan-Hunter substance P as radioligand B 7.49 pIC50 32 nM IC50 J. Med. Chem. (1996) 39: 736-748 [PMID:8576917]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]