GR 159897 [Ligand Id: 2115] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2110370 (GR-159897)
  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
  • NK2 receptor/Neurokinin 2 receptor in Rat [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
1 CHEMBL2110370_lig_chart_1 Neurokinin 2 receptor HumanRat
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  • Neurokinin 3 receptor in Guinea pig [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
  • This target only has 1 pki data point
2 CHEMBL2110370_lig_chart_2 Neurokinin 3 receptor Guinea pig
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
GtoPdb - - 9.5 pKd - - - Biochem. Biophys. Res. Commun. (1993) 191: 1172-7 [PMID:7682062];
J. Med. Chem. (1995) 38: 3772-9 [PMID:7562907];
Eur. J. Pharmacol. (1995) 272: 241-8 [PMID:7713168]
ChEMBL Binding affinity against Tachykinin receptor 2 of human expressed in chinese hamster ovary cells B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 1951-1956
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
ChEMBL Binding affinity by displacement of radiolabeled GR-100679 from Tachykinin receptor 2 from homogenized rat colon B 10 pKi 0.1 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 1951-1956
Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
ChEMBL Tested for inhibition of binding of [3H]senktide to Tachykinin receptor 3 in guinea pig cerebral cortex membranes B 4.7 pKi 19952.62 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 1951-1956

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]