ChEMBL ligand: CHEMBL80 (Dbl naloxone, Nalone, Naloxone, Narcan, Narcanti, NSC-70413, Suboxone)
A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] There should be some charts here, you may need to enable JavaScript!
CCR5/C-C chemokine receptor type 5 in Mouse [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682] There should be some charts here, you may need to enable JavaScript!
CYP2D6/Cytochrome P450 2D6 in Human [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] There should be some charts here, you may need to enable JavaScript!
δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] There should be some charts here, you may need to enable JavaScript!
D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] There should be some charts here, you may need to enable JavaScript!
κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] κ receptor/Kappa opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144] There should be some charts here, you may need to enable JavaScript!
μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] Mu opioid receptor in Bovine [ChEMBL: CHEMBL3041] [UniProtKB: P79350] μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] 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
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL	Binding affinity to adenosine receptor A1	B	4.3	pKi	>50000	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950]
CCR5/C-C chemokine receptor type 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682]
ChEMBL	Binding affinity to CCR5 in C57BL/6J mouse brain membrane	B	7.68	pKd	20.8	nM	Kd	Proc Natl Acad Sci U S A (2007) 104: 6061-6065 [PMID:17389363]
ChEMBL	Binding affinity to CCR5 in NY1DD transgenic mouse brain membrane	B	7.98	pKd	10.5	nM	Kd	Proc Natl Acad Sci U S A (2007) 104: 6061-6065 [PMID:17389363]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL	DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)	B	5.7	pIC50	2000	nM	IC50	DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL	Displacement of [3H]DPDPE from human DOR expressed in HEK293 cells after 60 mins by scintillation counting analysis	B	5.82	pKi	1516	nM	Ki	J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL	DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)	B	6.29	pKi	515	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells	B	6.92	pKi	120	nM	Ki	Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL	Displacement of [3H]diprenorphine human delta opioid receptor expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method	B	6.92	pKi	120	nM	Ki	ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376]
ChEMBL	Displacement of [3H]deltrophine from human delta opioid receptor expressed in CHO-K1 cells after 120 mins by liquid scintillation counting method	B	6.99	pKi	103	nM	Ki	Medchemcomm (2016) 7: 317-326
ChEMBL	Displacement of [3H]-deltorphine from human delta opioid receptor expressed in CHO-K1 cells by scintillation counting analysis	B	6.99	pKi	103	nM	Ki	J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL	Displacement of [3H]-diprenorphine from human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by competition radioligand binding assay	B	7.01	pKi	98.1	nM	Ki	J Med Chem (2020) 63: 7663-7694 [PMID:32530286]
ChEMBL	Displacement of [3H]naltrindole from human opioid delta receptor expressed in CHO cells	B	7.12	pKi	76	nM	Ki	J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL	Displacement of [3H]-diprenorphine from human DOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method	B	7.14	pKi	72.8	nM	Ki	J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL	Displacement of [3H]-diprenorphine from human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method	B	7.15	pKi	70	nM	Ki	ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL	Displacement of [125I]OXY from human delta opioid receptor expressed in CHO cells	B	7.29	pKi	51	nM	Ki	J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL	Displacement of [3H]DPDPE from delta opioid receptor	B	7.37	pKi	42.6	nM	Ki	J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL	Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (2000) 10: 523-526 [PMID:10741545]
ChEMBL	Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cells after 3 hrs by scintillation counting	B	7.42	pKi	38	nM	Ki	Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
ChEMBL	In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement.	B	7.43	pKi	37	nM	Ki	J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL	Concentration required to inhibit the binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human delta opioid receptor	B	7.48	pKi	33	nM	Ki	Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL	Displacement of [3H]diprenorphine from human cloned delta opioid receptor	B	7.48	pKi	33	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL	Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells	B	7.48	pKi	33	nM	Ki	J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL	Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells	B	7.48	pKi	33	nM	Ki	J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL	Displacement of [3H]DPDPE from delta opioid receptor (unknown origin) transfected into HEK293 cells by microplate scintillation counting	B	7.52	pKi	30	nM	Ki	J Nat Prod (2015) 78: 1461-1465 [PMID:26035635]
ChEMBL	Displacement of [3H]DPN from human recombinant delta-type opioid receptor expressed in CHO cell membranes	B	7.67	pKi	21.38	nM	Ki	Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]
ChEMBL	In vivo binding affinity against delta Opioid receptor was measured by using labeled ligand [3H]DADLE (1 nM) with 4 nM sufentanil	B	7.72	pKi	19	nM	Ki	J Med Chem (1994) 37: 3121-3127 [PMID:7932535]
ChEMBL	Binding affinity to delta-opioid receptor (unknown origin)	B	7.8	pKi	15.85	nM	Ki	J Nat Prod (2021) 84: 713-723 [PMID:32870011]
ChEMBL	DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)	B	5.84	pIC50	1461	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr	F	6.82	pIC50	153	nM	IC50	J Med Chem (2020) 63: 7663-7694 [PMID:32530286]
ChEMBL	Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand	B	6.82	pIC50	151	nM	IC50	J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL	Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr	F	6.84	pIC50	146	nM	IC50	ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL	Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membrane	B	6.86	pIC50	138	nM	IC50	J Nat Prod (2007) 70: 866-868 [PMID:17388627]
ChEMBL	Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells	B	6.86	pIC50	138	nM	IC50	J Nat Prod (2007) 70: 1946-1950 [PMID:18039010]
ChEMBL	Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK293 cells	B	6.86	pIC50	138	nM	IC50	J Nat Prod (2006) 69: 1295-1299 [PMID:16989522]
ChEMBL	Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membranes	B	6.86	pIC50	138	nM	IC50	J Nat Prod (2007) 70: 872-875 [PMID:17451272]
ChEMBL	Antagonist activity at human DOR expressed in CHO cell membranes assessed as reduction in SNC80-induced response incubated for 1 hr by [35S]-GTPgammaS coupling assay	F	7.11	pIC50	78.2	nM	IC50	J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL	Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane	B	7.21	pIC50	62	nM	IC50	J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL	Inhibition of [3H]DPDPE binding to guinea pig brain membrane Opioid receptor delta 1 at 1.0 nM	B	7.21	pIC50	62	nM	IC50	J Med Chem (1992) 35: 2374-2384 [PMID:1320121]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL	Tested for inhibitory activity against (DPDE)delta receptor in mouse vas deferens	B	7.3	pKd	50.12	nM	Kd	J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL	Antagonist activity at delta opioid receptor in Swiss mouse vas deferens assessed as reversal of DSLET effect on electrically-induced driven twitch	F	7.35	pKd	44.67	nM	Kd	Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL	Affinity against the Opioid receptor delta 1	B	7.74	pKd	18	nM	Kd	J Med Chem (1986) 29: 531-537 [PMID:3007760]
ChEMBL	Displacement of [3H]DPDPE from DOR in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting method	B	6.99	pKi	103	nM	Ki	J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL	Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates	B	7.49	pKi	32	nM	Ki	J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
ChEMBL	Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794]
ChEMBL	Displacement of [3H]DPDPE from delta opioid receptor in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting analysis	B	8.62	pKi	2.4	nM	Ki	Medchemcomm (2016) 7: 2368-2380
ChEMBL	Displacement of [3H]DPDPE from delta opioid receptor in rat membranes after 120 mins by scintillation counting analysis	B	8.62	pKi	2.4	nM	Ki	J Med Chem (2019) 62: 4204-4217 [PMID:30939014]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL	Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.	B	4.7	pKi	>20000	nM	Ki	J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL	Displacement of [3H]U-69593 from human KOR expressed in HEK293 cells after 60 mins by scintillation counting analysis	B	6.44	pKi	362	nM	Ki	J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL	DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)	B	7.52	pKi	30	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to kappa-opioid receptor (unknown origin)	B	7.8	pKi	15.85	nM	Ki	J Nat Prod (2021) 84: 713-723 [PMID:32870011]
ChEMBL	Displacement of [3H]Cl-977 from human kappa opioid receptor expressed on HEK-293 cells by liquid scintillation counting method	B	7.82	pKi	15	nM	Ki	Medchemcomm (2016) 7: 317-326
ChEMBL	Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells	B	7.83	pKi	14.7	nM	Ki	J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL	In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement.	B	7.97	pKi	10.7	nM	Ki	J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor	B	8.04	pKi	9.2	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL	Binding affinity at cloned human kappa opioid receptor by [3H]diprenorphine displacement.	B	8.04	pKi	9.2	nM	Ki	Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells	B	8.04	pKi	9.2	nM	Ki	J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells	B	8.04	pKi	9.2	nM	Ki	J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL	Displacement of [3H]DPN from human recombinant kappa-type opioid receptor expressed in CHO cell membranes	B	8.35	pKi	4.47	nM	Ki	Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]
ChEMBL	Displacement of [125I]OXY from human kappa opioid receptor expressed in CHO cells	B	8.52	pKi	3	nM	Ki	J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL	Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells	B	8.92	pKi	1.2	nM	Ki	Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL	Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 expressed in HEK 293 cells	B	8.92	pKi	1.2	nM	Ki	Bioorg Med Chem Lett (2000) 10: 523-526 [PMID:10741545]
ChEMBL	Displacement of [3H]U-69593 from human opioid kappa receptor expressed in CHO cells	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL	Displacement of [3H]U69563 from human kappa-opioid receptor expressed in CHO cells after 60 mins by scintillation counting	B	9.6	pKi	0.25	nM	Ki	Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
ChEMBL	Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding	F	6.49	pIC50	320	nM	IC50	J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL	Antagonist activity at human KOR expressed in CHO cell membranes assessed as reduction in U50,488 induced response incubated for 1 hr by liquid scintillation counting based [35S]GTP-gamma-S assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2016) 59: 10291-10298 [PMID:27797517]
ChEMBL	DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)	B	7.12	pIC50	75	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488	F	7.3	pIC50	49.8	nM	IC50	J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL	Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand	B	8.82	pIC50	1.5	nM	IC50	J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL	Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	F	8	pEC50	10	nM	EC50	J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL	Effective concentration for half-maximal stimulation was determined by [35S]GTP-gamma-S, assay	F	8.18	pEC50	6.6	nM	EC50	J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL	Antagonist activity at kappa opioid receptor in Swiss mouse vas deferens assessed as reversal of U50488 effect on electrically-induced driven twitch	F	6.9	pKd	125.89	nM	Kd	Bioorg Med Chem (2008) 16: 869-873 [PMID:17962026]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL	Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor kappa 1	B	8.35	pKd	4.5	nM	Kd	Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696]
ChEMBL	Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa)	B	9	pKd	1	nM	Kd	J Med Chem (1986) 29: 531-537 [PMID:3007760]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL	Tested for its antagonist activity against kappa receptor using U-69,593 as radioligand in isolated guinea pig ileum	F	7.7	pKd	19.95	nM	Kd	J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL	Binding affinity towards kappa-opioid receptor by displacement of [3H]-EKC at from guinea pig cortical tissue	B	7.18	pKi	66	nM	Ki	J Med Chem (1993) 36: 2833-2841 [PMID:8410998]
ChEMBL	Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue	B	7.18	pKi	66	nM	Ki	J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
ChEMBL	Tested for binding affinity towards kappa receptor in presence of [3H]EKC radioligand	B	7.18	pKi	66	nM	Ki	J Med Chem (1994) 37: 2262-2265 [PMID:8057274]
ChEMBL	Displacement of [3H]Cl-977 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis	B	7.82	pKi	15	nM	Ki	J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL	In vivo binding affinity against kappa opioid receptor was measured by using labeled ligand [3H]ethylketocyclazocine (1 nM) with 500 nM DADLE and 20 nM sufentanil	B	7.92	pKi	12	nM	Ki	J Med Chem (1994) 37: 3121-3127 [PMID:7932535]
ChEMBL	Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL	Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL	Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes after 150 mins by scintillation counting	B	8.14	pKi	7.3	nM	Ki	Eur J Med Chem (2011) 46: 1972-1982 [PMID:21481987]
ChEMBL	Displacement of [3H]U-69,593 from kappa-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
ChEMBL	Displacement of [3H]U-69,593 from KOR in guinea pig brain membranes after 120 mins by scintillation counting method	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL	Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting analysis	B	8.16	pKi	6.9	nM	Ki	J Med Chem (2019) 62: 4204-4217 [PMID:30939014]
ChEMBL	Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting	B	8.16	pKi	6.9	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794]
ChEMBL	Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane	B	8.16	pKi	6.9	nM	Ki	Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182]
ChEMBL	Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis	B	8.16	pKi	6.9	nM	Ki	Medchemcomm (2016) 7: 2368-2380
ChEMBL	Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes	B	8.49	pKi	3.2	nM	Ki	J Med Chem (2001) 44: 2814-2826 [PMID:11495592]
ChEMBL	Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane	B	8.5	pKi	3.17	nM	Ki	Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073]
ChEMBL	Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membarnes by liquid scintillation counting method	B	8.51	pKi	3.1	nM	Ki	Medchemcomm (2016) 7: 317-326
ChEMBL	Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane	B	7.3	pIC50	50	nM	IC50	J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL	Displacement of 0.5 nM [3H]bremazocine from guinea pig brain membrane opioid receptor kappa with 100 nM DAGO and 100 nM DPDPE	B	7.3	pIC50	50	nM	IC50	J Med Chem (1992) 35: 2374-2384 [PMID:1320121]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Antagonist activity against mu opioid receptor assessed as effect on endomorphin-2-induced calcium response in CHO cells by aequorin luminescence based calcium assay	F	9.66	pKd	0.22	nM	Kd	J Med Chem (2007) 50: 512-520 [PMID:17266203]
ChEMBL	Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	F	9.66	pKd	0.22	nM	Kd	Bioorg Med Chem Lett (2008) 18: 1350-1353 [PMID:18207400]
ChEMBL	Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 60 mins by scintillation counting analysis	B	6.45	pKi	354	nM	Ki	J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL	Displacement of [3H]-diprenorphine from human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by competition radioligand binding assay	B	7.23	pKi	59.5	nM	Ki	J Med Chem (2020) 63: 7663-7694 [PMID:32530286]
ChEMBL	Displacement of [3H]-diprenorphine from human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method	B	7.29	pKi	51.2	nM	Ki	ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL	Displacement of [3H]-diprenorphine from human MOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method	B	7.29	pKi	51	nM	Ki	J Med Chem (2020) 63: 2673-2687 [PMID:31834798]
ChEMBL	Displacement of [3H]diprenorphine human MOR expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method	B	7.37	pKi	43	nM	Ki	ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376]
ChEMBL	DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)	B	8.09	pKi	8.06	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells	B	8.37	pKi	4.23	nM	Ki	Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL	Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2006) 49: 7278-7289 [PMID:17149858]
ChEMBL	Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2006) 49: 7290-7306 [PMID:17149859]
ChEMBL	Inhibition of binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human mu opioid receptor	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem Lett (2003) 13: 4459-4462 [PMID:14643346]
ChEMBL	Displacement of [3H]diprenorphine from human cloned mu opioid receptor	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL	In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement.	B	8.44	pKi	3.63	nM	Ki	J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL	Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO-K1 cells by scintillation counting analysis	B	8.64	pKi	2.3	nM	Ki	J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL	Displacement of [3H]naloxone from human mu opioid receptor expressed in CHO-K1 cells after 150 mins by liquid scintillation counting method	B	8.64	pKi	2.3	nM	Ki	Medchemcomm (2016) 7: 317-326
ChEMBL	Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells	B	8.64	pKi	2.27	nM	Ki	Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL	Displacement of [3H]DAGO from mu opioid receptor	B	8.8	pKi	1.6	nM	Ki	J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL	Binding affinity to mu opioid receptor	B	8.82	pKi	1.5	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950]
ChEMBL	Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis	B	8.9	pKi	1.26	nM	Ki	J Med Chem (2015) 58: 9754-9767 [PMID:26632862]
ChEMBL	Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexyl)-amino)-6-oxohexyl)-3,3-dimethyl-3H-indol-1-ium-5-sulfonate,2,2,2-Trifluoroacetate Salt from human MOR expressed in HEK293 cells by Cheng-Prusoff analysis	B	8.94	pKi	1.15	nM	Ki	J Med Chem (2015) 58: 9754-9767 [PMID:26632862]
ChEMBL	Binding affinity to mu-opioid receptor (unknown origin)	B	9	pKi	1	nM	Ki	J Nat Prod (2021) 84: 713-723 [PMID:32870011]
ChEMBL	Displacement of [125I]OXY from human mu opioid receptor expressed in CHO cells	B	9.01	pKi	0.98	nM	Ki	J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL	Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells	B	9.1	pKi	0.79	nM	Ki	J Med Chem (2007) 50: 2254-2258 [PMID:17407276]
ChEMBL