senktide [Ligand Id: 2127] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL106124 (Senktide) |
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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 | Displacement of [3H]-Substance P from human NK1R after 90 mins by scintillation counting analysis | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2015) 58: 3060-3082 [PMID:25738882] |
| ChEMBL | Inhibitory activity against Tachykinin receptor 1 in human lymphoma IM9 cells labeled with [125I]Bolton-Hunter substance P | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
| ChEMBL | Displacement of [125I]-BH-SP from NK1 receptor (unknown origin) expressed in CHO cells by scintillation counter | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2015) 6: 469-476 |
| Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547] | ||||||||
| ChEMBL | Effective concentration to activate Tachykinin receptor 1 in guinea pig ileum(GPI) | B | 4.46 | pEC50 | 35000 | nM | EC50 | J Med Chem (1996) 39: 3174-3178 [PMID:8759639] |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| ChEMBL | Displacement of [125I]NKA from human NK2R expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2015) 58: 3060-3082 [PMID:25738882] |
| ChEMBL | Displacement of [125I]-NKA from NK2 receptor (unknown origin) expressed in CHO cells by scintillation counter | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2015) 6: 469-476 |
| NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371] | ||||||||
| ChEMBL | Displacement of [125I][MePhe7]NKB from human NK3R expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2015) 58: 3060-3082 [PMID:25738882] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
J Biol Chem (1996) 271: 20250-7 [PMID:8702757]; J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866]; Eur J Pharmacol (2001) 413: 143-50 [PMID:11226387] |
| ChEMBL | Displacement of [125I]His3, MePhe7 from human NK3R expressed in CHO cell membranes by scintillation counting | B | 7.25 | pIC50 | 56 | nM | IC50 | J Med Chem (2014) 57: 8646-8651 [PMID:25247671] |
| ChEMBL | Displacement of ([125I]His3-MePhe7)-NKB from NK3 receptor (unknown origin) expressed in CHO cells by scintillation counter | B | 7.54 | pIC50 | 29 | nM | IC50 | Medchemcomm (2015) 6: 469-476 |
| ChEMBL | Inhibitory activity against Tachykinin receptor 3 in rat cortical membranes labeled with [125I][MePhe7]-NKB | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
| ChEMBL | Binding affinity towards human Tachykinin receptor 3 stably expressed in CHO cells using [125I][MePhe7]-NKB as radioligand | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1773-1778 |
| ChEMBL | Displacement of [125I][MePhe]-NKB from human NK3 receptor expressed in CHO cells | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1679-1684 |
| ChEMBL | Compound was evaluated for its ability to displace [3H]NKB binding in hNK3 receptors expressed in CHO cells | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| ChEMBL | Agonist activity at human NK3R expressed in CHO cells assessed as potentiation of senktide-induced effect | B | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2014) 57: 8646-8651 [PMID:25247671] |
| ChEMBL | Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells | F | 8.15 | pEC50 | 7 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| ChEMBL | Activity at human NK3 receptor expressed in CHO cells assessed as increase in inositol phosphate generation | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617] |
| NK3 receptor in Mouse [GtoPdb: 362] [UniProtKB: P47937] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | Eur J Pharmacol (2001) 413: 143-50 [PMID:11226387] |
| NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177] | ||||||||
| GtoPdb | - | - | 9.1 | pKd | 0.9 | nM | Kd |
J Biol Chem (1986) 261: 10257-63 [PMID:2426259]; FEBS Lett (1992) 299: 90-5 [PMID:1312036] |
| ChEMBL | Inhibitory activity against cloned human Tachykinin receptor 3 in CHO cells labeled with [125I][MePhe7]-NKB | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
| ChEMBL | Agonist activity at rat NK3R | B | 7.89 | pEC50 | 13 | nM | EC50 | J Med Chem (2014) 57: 8646-8651 [PMID:25247671] |
| GtoPdb | - | - | 8.8 | pEC50 | 1.5 | nM | EC50 | J Biol Chem (1986) 261: 10257-63 [PMID:2426259] |
| ChEMBL | Effective concentration to activate Tachykinin receptor 3 in rat portal vein (RPV) | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (1996) 39: 3174-3178 [PMID:8759639] |
| ChEMBL | Agonist activity at rat NK3 receptor expressed in CHO cells assessed as calcium influx relative to 100 nM senktide | F | 10.64 | pEC50 | 0.02 | nM | EC50 | Medchemcomm (2015) 6: 469-476 |
| Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098] | ||||||||
| ChEMBL | Inhibitory activity against Tachykinin receptor 3 in guinea pig cortical membranes labeled with [125I]-[MePhe7] | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
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]
