ChEMBL ligand: CHEMBL429731
NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6] There should be some charts here, you may need to enable JavaScript!
NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5] NPFF2 receptor/Neuropeptide FF receptor 2 in Mouse [ChEMBL: CHEMBL4523416] [GtoPdb: 301] [UniProtKB: Q924H0] NPFF2 receptor/Neuropeptide FF receptor 2 in Rat [ChEMBL: CHEMBL3425] [GtoPdb: 301] [UniProtKB: Q9EQD2] There should be some charts here, you may need to enable JavaScript!
MAS1 in Mouse [GtoPdb: 150] [UniProtKB: P30554] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
ChEMBL	Binding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay	B	8.95	pKd	1.13	nM	Kd	J Med Chem (2020) 63: 12387-12402 [PMID:32673481]
GtoPdb	-	-	9.9	pKi	-	-	-	Eur J Pharmacol (2002) 451: 245-56 [PMID:12242085]; Neuropharmacology (2007) 52: 376-86 [PMID:17011599]; Neuroscience (2002) 115: 349-61 [PMID:12421602]
ChEMBL	Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method	B	10.22	pKi	0.06	nM	Ki	J Med Chem (2021) 64: 7555-7564 [PMID:34008968]
ChEMBL	Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay	F	6.56	pEC50	275.42	nM	EC50	J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL	Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay	F	6.56	pEC50	274	nM	EC50	J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL	Agonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	F	6.8	pEC50	158.49	nM	EC50	Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554]
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
ChEMBL	Binding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay	B	9.43	pKd	0.37	nM	Kd	J Med Chem (2020) 63: 12387-12402 [PMID:32673481]
ChEMBL	Binding affinity to human NPFFR2	B	9.68	pKd	0.21	nM	Kd	J Med Chem (2020) 63: 12387-12402 [PMID:32673481]
ChEMBL	Displacement of [3H]EYE from human NPFF2 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrophotometric counting	B	8.92	pKi	1.2	nM	Ki	J Med Chem (2016) 59: 1925-1945 [PMID:26824643]
GtoPdb	-	-	9.7	pKi	-	-	-	Neuroscience (2002) 115: 349-61 [PMID:12421602]; Br J Pharmacol (2001) 133: 1-4 [PMID:11325787]
ChEMBL	Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method	B	10.7	pKi	0.02	nM	Ki	J Med Chem (2021) 64: 7555-7564 [PMID:34008968]
ChEMBL	Agonist activity at human NPFF2 receptor E5.27A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	F	6.21	pEC50	612	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL	Agonist activity at human NPFF2 receptor D6.59A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	F	6.47	pEC50	341	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL	Agonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	F	6.9	pEC50	126	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
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	6.92	pEC50	119	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL	Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay	F	7.37	pEC50	42.66	nM	EC50	J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL	Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay	F	7.37	pEC50	42.4	nM	EC50	J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL	Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	F	7.4	pEC50	39.81	nM	EC50	Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554]
ChEMBL	Agonist activity at human NPFF2 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	F	7.48	pEC50	33	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL	Agonist activity at human NPFF2 receptor F5.34A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	F	8.25	pEC50	5.6	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL	Agonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cyclic cAMP accumulation	F	8.5	pEC50	3.16	nM	EC50	J Med Chem (2020) 63: 12387-12402 [PMID:32673481]
ChEMBL	Agonist activity at human NPFF2 receptor H/Q6.69A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	F	8.57	pEC50	2.7	nM	EC50	J Med Chem (2012) 55: 6124-6136 [PMID:22708927]
NPFF2 receptor/Neuropeptide FF receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523416] [GtoPdb: 301] [UniProtKB: Q924H0]
ChEMBL	Displacement of [125I]-1DMeNPFF from mouse NPFF2R receptor by TopCount scintillation counting method	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2021) 64: 7555-7564 [PMID:34008968]
NPFF2 receptor/Neuropeptide FF receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3425] [GtoPdb: 301] [UniProtKB: Q9EQD2]
ChEMBL	Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF	B	9.68	pKi	0.21	nM	Ki	J Med Chem (1994) 37: 3477-3481 [PMID:7932576]
MAS1 in Mouse [GtoPdb: 150] [UniProtKB: P30554]
GtoPdb	-	-	6.4	pEC50	400	nM	EC50	Cell (2001) 106: 619-32 [PMID:11551509]

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]