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 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]
