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 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]
