RP67580 [Ligand Id: 3522] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL131171 (RP-67580) |
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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 | Compound was tested for its binding affinity to NK1 receptor in [3H]SP binding assay on human IM9 lymphoblasts cultured cell line. | B | 7.31 | pIC50 | 49 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1591-1594 |
| ChEMBL | Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
| GtoPdb | - | - | 7.7 | pIC50 | - | - | Ki | J Biol Chem (1992) 267: 25668-71 [PMID:1281470] |
| NK1 receptor/Neurokinin 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2668] [GtoPdb: 360] [UniProtKB: P30548] | ||||||||
| ChEMBL | Inhibitory activity against Tachykinin receptor 1 in mouse brain using [125I]-labeled Boltan-Hunter substance P as radioligand | B | 8.06 | pIC50 | 8.7 | nM | IC50 | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Tested for binding affinity towards Tachykinin receptor 1 by using [3H]SP binding assay in rat brain membranes | B | 8.38 | pKi | 4.16 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 37-40 |
| ChEMBL | Inhibition of [3H]SP binding in rat brain membranes | B | 5.38 | pIC50 | 4160 | nM | IC50 | J Med Chem (1995) 38: 4793-4805 [PMID:7490729] |
| ChEMBL | Compound was tested for its binding affinity to NK1 receptor in [3H]SP binding assay on rat brain membranes. | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1591-1594 |
| ChEMBL | Inhibitory activity against Tachykinin receptor 1 in rat brain using [125I]-labeled Boltan-Hunter substance P as radioligand | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
| Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547] | ||||||||
| ChEMBL | Tested for inhibition of contractile effects of Tachykinin receptor 1 in guinea pig ileum preparation. | F | 7.2 | pKd | 63.1 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 37-40 |
| ChEMBL | Inhibitory activity against Tachykinin receptor 1 in guinea pig brain using [125I]-labeled Boltan-Hunter substance P as radioligand | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
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]
