[3H]saredutant [Ligand Id: 3481] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL308148 (Saredutant)
  • NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
  • NK1 receptor/Neurokinin 1 receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
  • This target only has 1 pki data point
1 CHEMBL308148_lig_chart_1 Neurokinin 1 receptor HumanRat
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2 CHEMBL308148_lig_chart_2 Neurokinin 2 receptor HumanBovineHamsterRat
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  • Neurokinin 3 receptor in Guinea pig [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
  • This target only has 0 pki data point
3 CHEMBL308148_lig_chart_3 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
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined B 6.1 pIC50 800 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2259-2262 [PMID:9873524]
ChEMBL Binding affinity against Neurokinin 1(NK1) receptor from human IM-9 cells using [I]-Bolton Hunter labeled SP B 6.23 pIC50 593 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 951-956
NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
ChEMBL Tested in vitro to inhibit the binding of [125I]NKA to its receptor in rat duodenum membrane B 9.29 pKi 0.51 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 319-322
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Binding affinity towards Tachykinin receptor 2 in CHO cells using [3H]-neurokinin A as radioligand B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2329-2332 [PMID:11055349]
ChEMBL Binding affinity was determined against human NK2 receptor in CHO cells using [125I]neurokinin A as radioligand B 9.1 pIC50 0.8 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 605-608
ChEMBL Binding affinity against human NK2 receptors from HSKR-1 cells using [125I]-Iodohistidyl NKA B 9.36 pIC50 0.44 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 951-956
ChEMBL Inhibition of cloned human NK2 (Neurokinin 2) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined B 9.89 pIC50 0.13 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2259-2262 [PMID:9873524]
Neurokinin 2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4815] [UniProtKB: P05363]
ChEMBL Binding affinity against bovine Tachykinin receptor 2 B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4779-4782 [PMID:15324907]
Neurokinin 2 receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304405] [UniProtKB: P51144]
ChEMBL The compound was evaluated for the inhibition of [125I]NKA binding to neurokinin NK2 receptor from hamster urinary bladder membranes B 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 925-930
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
GtoPdb - - 9.7 pKd 0.2 nM Kd Recept. Channels (1994) 2: 295-302 [PMID:7719707]
ChEMBL The compound was evaluated for the inhibition of [125I]NKA binding to Tachykinin receptor 2 from rat duodenum membranes B 6.02 pKi 945 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 925-930
ChEMBL Inhibition of [125I]NKA binding to neurokinin NK2 receptor from rat duodenum membranes B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 925-930
Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
ChEMBL NK3 IC50 determined using [125I]bolton Hunter labeled eledoisin at NK3 receptors from guinea pig cerebral cortex B 6.68 pIC50 208 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 951-956

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]