neurokinin B [Ligand Id: 2090] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL437797 |
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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 | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2015) 58: 3060-3082 [PMID:25738882] |
| GtoPdb | - | - | 6.4 | pKi | - | - | - | J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866] |
| ChEMBL | Inhibitory activity against Tachykinin receptor 1 in human lymphoma IM9 cells labeled with [125 I] Bolton-Hunter substance P | B | 7.01 | pIC50 | 98 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
| ChEMBL | Inhibitory activity against binding of [125I]Bolton-Hunter SP to tachykinin NK-1 receptor in human lymphoma IM9 cells. | B | 7.01 | pIC50 | 97.5 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 165-166 |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Tested for inhibition of tachykinin 1 (NK1) receptor in rat brain synaptosomal membranes using [125I]BH-SP as radioligand | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 447-450 |
| ChEMBL | Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes was determined by using 125 [I]-BHSP as radioligand | B | 7.16 | pIC50 | 69 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 559-564 |
| Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547] | ||||||||
| ChEMBL | Binding affinity towards Tachykinin receptor 1 binding in guinea pig cerebral cortex membranes was determined using [3H]SP as the radioligand | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 559-564 |
| ChEMBL | In vitro agonistic activity against tachykinin receptor 1 of guinea pig ileum longitudinal smooth muscle. | F | 7.17 | pEC50 | 68 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| ChEMBL | The compound was tested for competition binding with [3H]NKA against the CHO cells from cloned human Tachykinin receptor 2 | B | 7.37 | pKi | 42.2 | nM | Ki | J Med Chem (1999) 42: 3004-3007 [PMID:10425111] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - |
J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866]; Biochem Biophys Res Commun (1993) 191: 1172-7 [PMID:7682062] |
| ChEMBL | Displacement of [125I]NKA from human NK2R expressed in CHO cell membranes after 90 mins by scintillation counting analysis | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (2015) 58: 3060-3082 [PMID:25738882] |
| ChEMBL | Inhibitory activity against human Tachykinin receptor 2 | B | 6.99 | pIC50 | 102.33 | nM | IC50 | J Med Chem (1999) 42: 3004-3007 [PMID:10425111] |
| Neurokinin 2 receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304405] [UniProtKB: P51144] | ||||||||
| ChEMBL | Competitive inhibition of [125I]NKA binding to hamster urinary bladder Tachykinin receptor 2 | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1992) 35: 3949-3955 [PMID:1331450] |
| ChEMBL | Inhibitory activity against Tachykinin receptor 2 in membranes prepared from hamster urinary bladder labeled with [125 I] NKA | B | 8.44 | pIC50 | 3.6 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
| NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610] | ||||||||
| ChEMBL | In vitro agonistic activity against tachykinin receptor 2 of rat colon muscularis mucosae. | F | 7.57 | pEC50 | 27 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| 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 | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2015) 58: 3060-3082 [PMID:25738882] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
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)-NKB from NK3R (unknown origin) transfected in CHO cells by gamma counting analysis | B | 7.12 | pIC50 | 76 | nM | IC50 | Bioorg Med Chem (2013) 21: 2413-2417 [PMID:23473945] |
| ChEMBL | Binding affinity towards human Tachykinin receptor 3 stably expressed in CHO cells using [125I][MePhe7]-NKB as radioligand | B | 8 | pIC50 | 10 | 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 | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1679-1684 |
| ChEMBL | Inhibitory activity against cloned human Tachykinin receptor 3 in CHO cells labeled with [125I][MePhe7]-NKB | B | 8.01 | pIC50 | 9.7 | nM | IC50 | J Med Chem (1996) 39: 1664-1675 [PMID:8648606] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]NKB binding in hNK3 receptors expressed in CHO cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| ChEMBL | Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| GtoPdb | - | - | 8.4 | pEC50 | 4 | nM | EC50 |
FEBS Lett (1992) 299: 90-5 [PMID:1312036]; Regul Pept (1990) 31: 125-35 [PMID:2176308] |
| NK3 receptor in Mouse [GtoPdb: 362] [UniProtKB: P47937] | ||||||||
| GtoPdb | - | - | 8.7 | 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] | ||||||||
| ChEMBL | In vitro agonistic activity against tachykinin receptor 3 of everted rat protal vein. | F | 8.2 | pEC50 | 6.3 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098] | ||||||||
| ChEMBL | Inhibitory activity against binding of [125I][MePhe7]-NKB SP to tachykinin NK-3 receptor in guinea pig cortical membranes. | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 165-166 |
| ChEMBL | Inhibitory activity against Tachykinin receptor 3 in guinea pig cortical membranes labeled with [125 I][MePhe7]-NKB | B | 8.7 | pIC50 | 2 | 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]
