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 [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 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 B 6.39 pIC50 410 nM IC50 Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554]
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 [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 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]