[3H]saredutant [Ligand Id: 3481] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL308148 (Saredutant, Sr-48968) |
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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 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]
