ChEMBL ligand: CHEMBL429731
δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] There should be some charts here, you may need to enable JavaScript!
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
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL	Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	F	6.92	pEC50	121.2	nM	EC50	J Med Chem (2023) 66: 17138-17154 [PMID:38095323]
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) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	F	7.1	pEC50	78.9	nM	EC50	J Med Chem (2023) 66: 17138-17154 [PMID:38095323]
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 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]