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ChEMBL ligand: CHEMBL1672380 (1-Adamantanecarbonyl-RF-NH2) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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MRGPRX1/Mas-related G-protein coupled receptor member X1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5850] [GtoPdb: 156] [UniProtKB: Q96LB2] | ||||||||
ChEMBL | Agonist activity at human MrgX1 transfected in HEK293 cells by FLIPR assay | B | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem (2014) 22: 5831-5837 [PMID:25288495] |
Mas-related G-protein coupled receptor member X1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3341576] [UniProtKB: Q8CIP3] | ||||||||
ChEMBL | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | B | 6.5 | pEC50 | 316.23 | nM | EC50 | Bioorg Med Chem (2014) 22: 5831-5837 [PMID:25288495] |
Mas-related G-protein coupled receptor member X1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3341575] [UniProtKB: Q8R4G1] | ||||||||
ChEMBL | Agonist activity at rat MrgX1 transfected in HEK293 cells by FLIPR assay | B | 5.2 | pEC50 | 6309.57 | nM | EC50 | Bioorg Med Chem (2014) 22: 5831-5837 [PMID:25288495] |
kisspeptin receptor/Metastin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5413] [GtoPdb: 266] [UniProtKB: Q969F8] | ||||||||
ChEMBL | Displacement of [125I]kisspeptin-15 from GPR54 | B | 6.08 | pIC50 | 830 | nM | IC50 | ACS Med Chem Lett (2011) 2: 53-57 [PMID:24900254] |
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - | Proc Natl Acad Sci USA (2006) 103: 466-71 [PMID:16407169] |
ChEMBL | Displacement of [125I]YVP from human NPFFR1 expressed in CHO cells | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2020) 63: 12387-12402 [PMID:32673481] |
ChEMBL | Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 7471-7474 [PMID:23131340] |
ChEMBL | Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2021) 64: 7555-7564 [PMID:34008968] |
ChEMBL | Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins | F | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554] |
ChEMBL | Antagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting method | F | 5.33 | pEC50 | 4700 | nM | EC50 | J Med Chem (2020) 63: 12387-12402 [PMID:32673481] |
ChEMBL | Agonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting | F | 6.34 | pEC50 | 462 | nM | EC50 | J Med Chem (2012) 55: 6124-6136 [PMID:22708927] |
ChEMBL | Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting | F | 7.15 | pEC50 | 71 | nM | EC50 | J Med Chem (2012) 55: 6124-6136 [PMID:22708927] |
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5] | ||||||||
GtoPdb | - | - | 7.1 | pKi | - | - | - | Proc Natl Acad Sci USA (2006) 103: 466-71 [PMID:16407169] |
ChEMBL | Displacement of [125I]Tyr-NPFF from human NPFFR2 expressed in green monkey Cos-1 cells | B | 7.12 | pKi | 75 | nM | Ki | J Med Chem (2020) 63: 12387-12402 [PMID:32673481] |
ChEMBL | Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 7471-7474 [PMID:23131340] |
ChEMBL | Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2021) 64: 7555-7564 [PMID:34008968] |
ChEMBL | Antagonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins | F | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554] |
ChEMBL | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting | F | 6.33 | pEC50 | 472 | nM | EC50 | J Med Chem (2012) 55: 6124-6136 [PMID:22708927] |
ChEMBL | Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting | F | 6.42 | pEC50 | 379 | nM | EC50 | J Med Chem (2012) 55: 6124-6136 [PMID:22708927] |
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]