RF9 [Ligand Id: 1486] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1672380 (1-Adamantanecarbonyl-RF-NH2)
  • MRGPRX1/Mas-related G-protein coupled receptor member X1 in Human [ChEMBL: CHEMBL5850] [GtoPdb: 156] [UniProtKB: Q96LB2]
  • Mas-related G-protein coupled receptor member X1 in Mouse [ChEMBL: CHEMBL3341576] [UniProtKB: Q8CIP3]
  • Mas-related G-protein coupled receptor member X1 in Rat [ChEMBL: CHEMBL3341575] [UniProtKB: Q8R4G1]
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  • kisspeptin receptor/Metastin receptor in Human [ChEMBL: CHEMBL5413] [GtoPdb: 266] [UniProtKB: Q969F8]
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  • NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
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  • NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]