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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
