ChEMBL ligand: CHEMBL567175 (Naltrindole)
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!
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] 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!
NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] 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	Antagonist activity against delta opioid receptor assessed as effect on deltorphin-2-induced calcium response in CHO cells by aequorin luminescence based calcium assay	F	7.95	pKd	11.22	nM	Kd	J Med Chem (2007) 50: 512-520 [PMID:17266203]
ChEMBL	Binding affinity to DOR (unknown origin) assessed as inhibition constant by radioligand binding assay	B	8.6	pKi	2.53	nM	Ki	Bioorg Med Chem Lett (2022) 72: 128860-128860 [PMID:35724925]
ChEMBL	Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells	B	8.71	pKi	1.97	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL	Displacement of [3H]DADLE from delta opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay	B	9.05	pKi	0.9	nM	Ki	Eur J Med Chem (2014) 85: 818-829 [PMID:25193297]
ChEMBL	Displacement of [3H]DADLE from delta opioid receptor (unknown origin)	B	9.05	pKi	0.9	nM	Ki	Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424]
ChEMBL	Displacement of [125I]-IBNalA from DOR-1 expressed in CHO cells	B	9.3	pKi	0.5	nM	Ki	Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL	Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells	B	9.34	pKi	0.46	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127176-127176 [PMID:32299730]
ChEMBL	Displacement of [125I]-IBNtxA from DOR-1 expressed in CHO cells	B	9.34	pKi	0.46	nM	Ki	Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL	Displacement of [3H]DPDPE from human DOR expressed in CHO cells	B	9.34	pKi	0.46	nM	Ki	Bioorg Med Chem Lett (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL	Binding affinity determined against Opioid receptor delta 1 from human cloned receptor	B	9.62	pKi	0.24	nM	Ki	J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL	Displacement of [3H]DADLE from Opioid receptor delta 1	B	9.66	pKi	0.22	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2883-2885 [PMID:11597422]
ChEMBL	Binding affinity towards recombinant human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta)	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2002) 45: 537-540 [PMID:11784158]
ChEMBL	Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes.	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL	Binding affinity for human Opioid receptor delta 1 transfected into chinese hamster ovary cells by displacing [3H]CI-DPDPE radioligand	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2003) 46: 3174-3177 [PMID:12825957]
ChEMBL	Inhibition of [3H]C1-DPDPE binding to human delta opioid receptor expressed in CHO cells	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL	Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cells	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2004) 47: 6645-6648 [PMID:15588100]
ChEMBL	Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method	B	9.7	pKi	0.2	nM	Ki	Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL	Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig	B	9.8	pKi	0.16	nM	Ki	J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL	Displacement of [3H]Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells after 60 mins	B	9.8	pKi	0.16	nM	Ki	Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL	Binding affinity to Opioid receptor delta 1 using [3H]DPDPE as a radioligand in guinea pig	B	9.82	pKi	0.15	nM	Ki	Bioorg Med Chem Lett (2001) 11: 939-943 [PMID:11294396]
ChEMBL	Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting	B	9.85	pKi	0.14	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL	Displacement of [3H]diprenorphine from human recombinant delta opioid receptor expressed in in CHO cells	B	9.97	pKi	0.11	nM	Ki	Bioorg Med Chem (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL	[3H]-Cl-DPDPE competition binding assay using human cloned opioid receptor delta 1	B	10.15	pKi	0.07	nM	Ki	J Med Chem (2004) 47: 281-284 [PMID:14711299]
ChEMBL	The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by SNC80 (Opioid receptor delta 1) antagonist	F	10.21	pKi	0.06	nM	Ki	J Med Chem (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL	Apparent antagonist activity determined by measuring the ability to inhibit stimulation of [35S]GTP-gamma-S, binding to opioid receptor delta 1 in guinea pig caudate membranes	F	10.21	pKi	0.06	nM	Ki	J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL	Ability to inhibit GTP-gamma-S binding to Opioid receptor delta 1 of guinea pig caudate.	B	10.21	pKi	0.06	nM	Ki	J Med Chem (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL	Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM SNC-80 as the agonist ligand for delta-receptor)	F	10.4	pKi	0.04	nM	Ki	Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL	Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes	B	10.51	pKi	0.03	nM	Ki	J Med Chem (1991) 34: 1757-1762 [PMID:1648136]
ChEMBL	Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 1	B	10.52	pKi	0.03	nM	Ki	J Med Chem (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL	The compound was evaluated for binding affinity against Opioid receptor delta 1 in guinea pig brain membrane using [3H]- DPDPE as ligand	B	10.52	pKi	0.03	nM	Ki	J Med Chem (1992) 35: 4325-4329 [PMID:1333013]
ChEMBL	The opioid receptor affinity(Ki) was evaluated by competition with [3H]-DPDPE (delta 1) on guinea pig brain membranes	B	10.52	pKi	0.03	nM	Ki	J Med Chem (1995) 38: 402-407 [PMID:7853332]
ChEMBL	Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of opioid receptor delta	B	10.52	pKi	0.03	nM	Ki	J Med Chem (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL	Displacement of [3H]Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells after 60 mins	B	9.04	pIC50	0.91	nM	IC50	Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL	Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as reduction in SNC80-induced inhibition of forskolin stimulated cAMP accumulation preincubated for 15 mins followed SNC80 and forskolin addition and measured after 10 mins relative to control	F	9.29	pIC50	<0.51	nM	IC50	ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778]
ChEMBL	Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding	F	9.41	pIC50	0.39	nM	IC50	Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL	Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane	B	9.49	pIC50	0.32	nM	IC50	J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL	Agonistic activity towards Opioid receptor delta 1	F	9.96	pEC50	0.11	nM	EC50	J Med Chem (2003) 46: 3174-3177 [PMID:12825957]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL	Displacement of deltorphin-II from delta opioid receptor in mouse vas deferens	B	9.2	pKd	0.63	nM	Kd	J Med Chem (2005) 48: 8035-8044 [PMID:16335927]
ChEMBL	Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells	B	8.74	pKi	1.82	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL	Binding affinity against Opioid receptor delta 1 using [3H][D-Ala2, D-Leu5]-enkephalin as radioligand	B	9.3	pKi	0.5	nM	Ki	J Med Chem (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL	Displacement of [3H]- diprenorphine from delta receptor expressed in HEK 293 cells	B	9.72	pKi	0.19	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL	Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum	B	9.77	pKi	0.17	nM	Ki	Bioorg Med Chem (2012) 20: 5810-5831 [PMID:22967810]
ChEMBL	Displacement of [3H]NTI from delta opioid receptor in CD1 mouse brain membranes	B	9.82	pKi	0.15	nM	Ki	J Med Chem (2007) 50: 2144-2156 [PMID:17402725]
ChEMBL	Binding affinity against Opioid receptor delta 1 receptor binding in ICR mouse brain membranes using the radioligand [3H]naltrindole	B	10.4	pKi	0.04	nM	Ki	J Med Chem (1997) 40: 1977-1981 [PMID:9207938]
ChEMBL	Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis	F	9.14	pIC50	0.72	nM	IC50	J Med Chem (2016) 59: 8381-8397 [PMID:27556704]
ChEMBL	Antagonist activity against Opioid receptor delta 1 in mouse vas deferens assay	F	9.2	pA2	9.2	nM	pA2	J Med Chem (1997) 40: 3100-3108 [PMID:9301674]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
GtoPdb	-	-	10.43	pKd	0.04	nM	Kd	Life Sci (1992) 50: PL119-24 [PMID:1313133]
ChEMBL	Displacement of [3H]DADLE from morphine-sensitive Opioid receptor delta 1 (presence of 300 nM DELT-II) of rat brain membranes	B	7.91	pKi	12.3	nM	Ki	J Med Chem (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL	Displacement of [3H]-(2-D-Ala)[Tyrosy1-3,5-]-DELTORPHIN II from Sprague-Dawley rat brain membrane delta opioid receptor incubated for 45 mins by liquid scintillation counting analysis	B	8.6	pKi	2.53	nM	Ki	Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113]
ChEMBL	Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane	B	8.8	pKi	1.6	nM	Ki	J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL	Displacement of [3H]DPDPE from DOR in rat brain membranes incubated for 45 mins by liquid scintillation counting	B	8.95	pKi	1.13	nM	Ki	Eur J Med Chem (2019) 168: 189-198 [PMID:30822708]
ChEMBL	Displacement of [3H]DPDPE from DOR in rat brain membranes incubated for 45 mins by liquid scintillation counting	B	9.08	pKi	0.83	nM	Ki	ACS Med Chem Lett (2020) 11: 678-685 [PMID:32435370]
ChEMBL	Binding affinity at delta opioid receptor 1 in rat brain membrane by [3H]DADLE displacement.	B	9.09	pKi	0.81	nM	Ki	J Med Chem (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL	Binding affinity for Opioid receptor delta 1 was determined by inhibition of binding of [3H]DADLE (1.3-2.0 nM) to rat brain membranes	B	9.39	pKi	0.41	nM	Ki	J Med Chem (1999) 42: 3527-3538 [PMID:10479286]
ChEMBL	Binding affinity to delta opioid receptor was measured using [3H]DADLE	B	9.39	pKi	0.41	nM	Ki	Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL	Compound was evaluated for the binding affinity towards Opioid receptor delta 1 in rat brain homogenates using [3H]naltrindole as radioligand	B	9.48	pKi	0.33	nM	Ki	Bioorg Med Chem Lett (1997) 7: 151-156
ChEMBL	Displacement of [3H]DADLE from delta opioid receptor in rat cerebellum membrane	B	9.54	pKi	0.29	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL	Displacement of [3H]DADLE from Opioid receptor delta 1 of rat brain membranes (DAMGO quenching mu receptor)	B	9.54	pKi	0.29	nM	Ki	J Med Chem (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL	Displacement of [3H]DADLE from delta opioid receptor in rat cerebrum membranes	B	9.54	pKi	0.29	nM	Ki	Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
ChEMBL	Displacement of [3H]DADLE from morphine-insensitive Opioid receptor delta 1 (presence of 50 nM morphine) of rat brain membranes	B	9.62	pKi	0.24	nM	Ki	J Med Chem (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL	Ability to displace [3H]DADLE radioligand from Opioid receptor delta 1	B	9.66	pKi	0.22	nM	Ki	J Med Chem (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL	Ability to displace [3H]DADL from delta opioid receptor	B	9.66	pKi	0.22	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL	Binding affinity to delta opioid receptor in rat brain membrane	B	9.66	pKi	0.22	nM	Ki	Eur J Med Chem (2008) 43: 2307-2315 [PMID:18403056]
ChEMBL	Binding affinity against Opioid receptor delta 1 from rat brain membranes using [3H]DADLE	B	9.66	pKi	0.22	nM	Ki	J Med Chem (2005) 48: 1620-1629 [PMID:15743203]
ChEMBL	Compound was tested for its ability to displace [3H]DADLE from delta receptor in rat brain.	B	9.66	pKi	0.22	nM	Ki	Bioorg Med Chem Lett (1998) 8: 799-804 [PMID:9871544]
ChEMBL	Displacement of [3H]p-Cl-DPDPE from rat delta opioid receptor expressed in rat C6 cells	B	9.7	pKi	0.2	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL	Tested for binding affinity against delta opioid receptor by displacing [3H]- DSLET radioligand from rat brain membrane preparations	B	9.74	pKi	0.18	nM	Ki	J Med Chem (1993) 36: 3182-3187 [PMID:8230106]
ChEMBL	Compound was evaluated for the binding affinity towards Opioid receptor delta 1 in rat brain homogenates using [3H]DIDI as radioligand	B	10.05	pKi	0.09	nM	Ki	Bioorg Med Chem Lett (1997) 7: 151-156
ChEMBL	Ability to inhibit binding of SNC80 to delta opioid receptor	B	10.21	pKi	0.06	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL	Compound was evaluated for its ability to displace [3H]p-CI-DPDPE in C6 glioma cells expressing the cloned Opioid receptor delta 1	B	10.4	pKi	0.04	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2449-2451 [PMID:11078198]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL	Displacement of [3H]U50488 from human kappa opioid receptor expressed in CHO cells	B	7.12	pKi	75	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL	Displacement of [3H]U-69593 from Opioid receptor kappa 1	B	7.52	pKi	30	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2883-2885 [PMID:11597422]
ChEMBL	Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells	B	7.83	pKi	14.7	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127176-127176 [PMID:32299730]
ChEMBL	Displacement of [3H]U-69,593 from human KOR expressed in CHO cells	B	7.83	pKi	14.7	nM	Ki	Bioorg Med Chem Lett (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL	Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells	B	8	pKi	10.1	nM	Ki	J Med Chem (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL	Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method	B	8	pKi	10.1	nM	Ki	Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL	Displacement of [3H]U-69593 from human recombinant kappa opioid receptor expressed in CHO cells	B	8	pKi	10.1	nM	Ki	J Med Chem (2004) 47: 6645-6648 [PMID:15588100]
ChEMBL	Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes.	B	8	pKi	10.1	nM	Ki	J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL	Binding affinity in recombinant human Opioid receptor kappa 1 transfected into chinese hamster ovary cells by displacing [3H]U-69593 radioligand	B	8	pKi	10.1	nM	Ki	J Med Chem (2003) 46: 3174-3177 [PMID:12825957]
ChEMBL	Binding affinity towards recombinant human Opioid receptor kappa 1 transfected in to CHO cells for the displacement of [3H]U-69593	B	8	pKi	10.1	nM	Ki	J Med Chem (2002) 45: 537-540 [PMID:11784158]
ChEMBL	Binding affinity against opioid receptor kappa 1 from human cloned receptor	B	8.36	pKi	4.4	nM	Ki	J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL	Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting	B	8.54	pKi	2.9	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL	Agonistic activity towards Opioid receptor kappa 1	F	8.31	pEC50	4.95	nM	EC50	J Med Chem (2003) 46: 3174-3177 [PMID:12825957]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL	Binding affinity against Opioid receptor kappa 1 binding in ICR mouse brain membranes using the radioligand [3H]U-69593	B	6.45	pKi	355	nM	Ki	J Med Chem (1997) 40: 1977-1981 [PMID:9207938]
ChEMBL	Binding affinity against Opioid receptor kappa 1 using [3H]-U-69,593 as radioligand	B	8.02	pKi	9.5	nM	Ki	J Med Chem (1997) 40: 3192-3198 [PMID:9379438]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL	Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells	B	7.38	pKi	42	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL	Binding affinity to kappa opioid receptor in rat brain membrane	B	7.52	pKi	30	nM	Ki	Eur J Med Chem (2008) 43: 2307-2315 [PMID:18403056]
ChEMBL	Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells	B	7.59	pKi	25.5	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL	Compound was evaluated for the binding affinity towards Opioid receptor kappa 1 in rat brain homogenates using [3H]CI977 as radioligand	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem Lett (1997) 7: 151-156
ChEMBL	Compound was evaluated for its ability to displace [3H]U-69593 in CHO cells expressing the cloned Opioid receptor kappa 1	B	8.24	pKi	5.8	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2449-2451 [PMID:11078198]
ChEMBL	Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells	B	8.91	pKi	1.23	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL	Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes	B	6.48	pKi	332	nM	Ki	J Med Chem (1991) 34: 1757-1762 [PMID:1648136]
ChEMBL	Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of opioid receptor kappa	B	6.48	pKi	332	nM	Ki	J Med Chem (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL	Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 1	B	6.48	pKi	332	nM	Ki	J Med Chem (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL	The opioid receptor affinity(Ki) was evaluated by competition with 9 (Opioid receptor kappa 1) on guinea pig brain membranes	B	6.48	pKi	332	nM	Ki	J Med Chem (1995) 38: 402-407 [PMID:7853332]
ChEMBL	The compound was evaluated for binding affinity against the opioid receptor kappa in guinea pig brain membranes using [3H]- U-69,593	B	6.48	pKi	332	nM	Ki	J Med Chem (1992) 35: 4325-4329 [PMID:1333013]
ChEMBL	Binding affinity against kappa-opioid receptor in guinea pig brain membranes	B	6.48	pKi	332	nM	Ki	J Med Chem (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL	Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes	B	7.12	pKi	75	nM	Ki	J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL	Binding affinity for Opioid receptor kappa 1 was determined by inhibition of binding of [3H]U-69593 (1.2-2.2 nM) to guinea pig brain membranes	B	7.45	pKi	35.8	nM	Ki	J Med Chem (1999) 42: 3527-3538 [PMID:10479286]
ChEMBL	Binding affinity for kappa opioid receptor was measured using [3H]U-69593	B	7.45	pKi	35.8	nM	Ki	Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL	Displacement of [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain membranes (pretreated with BIT and FIT to block mu and delta sites)	B	7.47	pKi	34.1	nM	Ki	J Med Chem (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL	Binding affinity to guinea pig kappa opioid receptor	B	7.52	pKi	30.4	nM	Ki	J Med Chem (2008) 51: 4404-4411 [PMID:18637671]
ChEMBL	Ability to displace [3H]U-69593 from kappa opioid receptor	B	7.52	pKi	30.4	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL	Compound was tested for its ability to displace [3H]U-69593 from kappa receptor in guinea pig brain.	B	7.52	pKi	30.4	nM	Ki	Bioorg Med Chem Lett (1998) 8: 799-804 [PMID:9871544]
ChEMBL	Ability to displace [3H]U-69593 radioligand from Opioid receptor kappa 1	B	7.52	pKi	30.4	nM	Ki	J Med Chem (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL	Binding affinity against Opioid receptor kappa 1 from guinea pig brain membranes using [3H]U-69593	B	7.57	pKi	26.92	nM	Ki	J Med Chem (2005) 48: 1620-1629 [PMID:15743203]
ChEMBL	Displacement of [125I]OXY from Opioid receptor kappa 2b of guinea pig brain membranes (pretreated with BIT(mu) and FIT(delta) and in the presence of (-)U50,488)	B	7.7	pKi	19.9	nM	Ki	J Med Chem (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL	Binding affinity at kappa opioid receptor 1 in guinea pig brain by [3H]U-69593 displacement.	B	7.8	pKi	15.8	nM	Ki	J Med Chem (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL	Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes	B	7.83	pKi	14.9	nM	Ki	J Med Chem (2007) 50: 2144-2156 [PMID:17402725]
ChEMBL	Binding affinity to Opioid receptor kappa 1 by using [3H]U-69593 as a radioligand from guinea pig	B	7.84	pKi	14.3	nM	Ki	Bioorg Med Chem Lett (2001) 11: 939-943 [PMID:11294396]
ChEMBL	Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum	B	7.85	pKi	14.01	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL	Tested for binding activity against kappa opioid receptor using [3H]U-69593 ligand	B	7.85	pKi	14	nM	Ki	J Med Chem (1994) 37: 579-585 [PMID:8126697]
ChEMBL	Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebrum membranes	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
ChEMBL	Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig	B	7.99	pKi	10.2	nM	Ki	J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL	Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum	B	8.04	pKi	9.04	nM	Ki	Bioorg Med Chem (2012) 20: 5810-5831 [PMID:22967810]
ChEMBL	The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by U69,593 (Opioid receptor kappa 1) antagonist	F	8.05	pKi	8.9	nM	Ki	J Med Chem (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL	Ability to inhibit GTP-gamma-S binding to Opioid receptor kappa 1 of guinea pig caudate.	B	8.05	pKi	8.85	nM	Ki	J Med Chem (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL	Ability to inhibit binding of U-69,593 to kappa opioid receptor	B	8.05	pKi	8.85	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL	Apparent binding affinity of compound was determined by antagonism towards Opioid receptor kappa 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate	F	8.06	pKi	8.8	nM	Ki	J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL	Displacement of [3H]DAMGO from kappa opioid receptor in Hartley guinea pig brain membrane	B	8.13	pKi	7.44	nM	Ki	J Med Chem (2008) 51: 4404-4411 [PMID:18637671]
ChEMBL	Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM U69,593 as the agonist ligand for kappa-receptor)	F	8.22	pKi	6	nM	Ki	Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL	Antagonist activity against kappa-opioid receptor in guinea pig ileum in the presence of ethylketazocine	F	5.7	pIC50	2000	nM	IC50	J Med Chem (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL	Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane	B	7	pIC50	100	nM	IC50	J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells	B	6.82	pKi	151	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4603-4606 [PMID:19595591]
ChEMBL	Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells	B	7.51	pKi	30.7	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127176-127176 [PMID:32299730]
ChEMBL	Displacement of [3H]DAMGO from human MOR expressed in CHO cells	B	7.51	pKi	30.7	nM	Ki	Bioorg Med Chem Lett (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL	Displacement of [3H]DAMGO from Opioid receptor mu 1	B	7.57	pKi	27	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2883-2885 [PMID:11597422]
ChEMBL	Tested for binding activity against mu opioid receptor using [3H]DAMGO ligand	B	7.84	pKi	14.4	nM	Ki	J Med Chem (1994) 37: 579-585 [PMID:8126697]
ChEMBL	Binding affinity determined against Opioid receptor mu 1 from human cloned receptor	B	8.14	pKi	7.2	nM	Ki	J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL	Inhibition of [3H]DAMGO binding to human Mu opioid receptor expressed in CHO cells	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL	Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2004) 47: 6645-6648 [PMID:15588100]
ChEMBL	Binding affinity towards recombinant human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]DAMGO (mu)	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2002) 45: 537-540 [PMID:11784158]
ChEMBL	Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL	Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes.	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL	Binding affinity for human Opioid receptor mu 1 transfected into chinese hamster ovary cells by displacing [3H]DAMGO radioligand	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2003) 46: 3174-3177 [PMID:12825957]
ChEMBL	Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting	B	8.28	pKi	5.3	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177]
ChEMBL	Effective concentration agonistic activity towards Opioid receptor mu 1	F	8.37	pEC50	4.26	nM	EC50	J Med Chem (2003) 46: 3174-3177 [PMID:12825957]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL	Binding affinity against Opioid receptor mu 1 using [3H][D-Ala2, MePhe4, Gly-ol5]-enkephalin as radioligand	B	7.82	pKi	15	nM	Ki	J Med Chem (1997) 40: 3192-3198 [PMID:9379438]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum	B	7.82	pKi	15	nM	Ki	Bioorg Med Chem (2012) 20: 5810-5831 [PMID:22967810]
ChEMBL	Binding affinity against Opioid receptor mu 1 binding in ICR mouse brain membranes using the radioligand [3H][Ala2,Glyol5]enkephalin	B	8.21	pKi	6.1	nM	Ki	J Med Chem (1997) 40: 1977-1981 [PMID:9207938]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL	Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane	B	6.82	pKi	151	nM	Ki	J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL	Binding affinity for Opioid receptor mu 1 was determined by inhibition of binding of [3H]DAMGO (1.4-3 nM) to rat brain membranes	B	7	pKi	99	nM	Ki	J Med Chem (1999) 42: 3527-3538 [PMID:10479286]
ChEMBL	Binding affinity to mu opioid receptor was measured using [3H]DAMGO	B	7	pKi	99	nM	Ki	Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL	Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes	B	7.3	pKi	50	nM	Ki	J Med Chem (1998) 41: 2872-2881 [PMID:9667975]
ChEMBL	Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells	B	7.46	pKi	34.4	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL	Compound was evaluated for the binding affinity towards mu opioid receptor in rat brain homogenates using [3H]DAMGO as radioligand	B	7.52	pKi	30.4	nM	Ki	Bioorg Med Chem Lett (1997) 7: 151-156
ChEMBL	Ability to displace [3H]DAMGO from mu opioid receptor	B	7.57	pKi	27	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL	Compound was tested for its ability to displace [3H]DAMGO from mu receptor in rat brain.	B	7.57	pKi	27	nM	Ki	Bioorg Med Chem Lett (1998) 8: 799-804 [PMID:9871544]
ChEMBL	Ability to displace [3H]DAMGO radioligand from Opioid receptor mu 1	B	7.57	pKi	27	nM	Ki	J Med Chem (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL	Binding affinity to mu opioid receptor in rat brain membrane	B	7.57	pKi	27	nM	Ki	Eur J Med Chem (2008) 43: 2307-2315 [PMID:18403056]
ChEMBL	Binding affinity against Opioid receptor mu 1 from rat brain membranes using [3H]DAMGO	B	7.57	pKi	26.92	nM	Ki	J Med Chem (2005) 48: 1620-1629 [PMID:15743203]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in rat cerebellum membrane	B	7.63	pKi	23.64	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in rat cerebrum membranes	B	7.63	pKi	23.6	nM	Ki	Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
ChEMBL	Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293	B	7.87	pKi	13.5	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL	Binding affinity at mu opioid receptor 1 in rat brain membrane by [3H]DAMGO displacement.	B	7.89	pKi	13	nM	Ki	J Med Chem (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL	Tested for binding affinity against mu opioid receptor fby displacing [3H]- DAMGO radioligand from rat brain membrane preparations	B	8.41	pKi	3.86	nM	Ki	J Med Chem (1993) 36: 3182-3187 [PMID:8230106]
ChEMBL	Compound was evaluated for its ability to displace [3H]DAMGO in C6 glioma cells expressing the cloned Opioid receptor mu 1	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2449-2451 [PMID:11078198]
ChEMBL	Ability to inhibit binding of [3H]DAMGO to mu opioid receptor	B	8.49	pKi	3.2	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3435-3438 [PMID:10617086]
ChEMBL	Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293	B	9.44	pKi	0.36	nM	Ki	J Med Chem (2001) 44: 857-862 [PMID:11300867]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL	Displacement of endomorphin-2 from mu opioid receptor in guinea pig ileum	B	7.3	pKd	50.12	nM	Kd	J Med Chem (2005) 48: 8035-8044 [PMID:16335927]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes	B	7.47	pKi	33.9	nM	Ki	J Med Chem (2007) 50: 2144-2156 [PMID:17402725]
ChEMBL	Binding affinity to Opioid receptor mu 1 by using [3H]DAMGO as a radioligand from guinea pig	B	7.56	pKi	27.5	nM	Ki	Bioorg Med Chem Lett (2001) 11: 939-943 [PMID:11294396]
ChEMBL	Binding affinity to guinea pig mu opioid receptor	B	7.57	pKi	27	nM	Ki	J Med Chem (2008) 51: 4404-4411 [PMID:18637671]
ChEMBL	Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig	B	7.83	pKi	14.7	nM	Ki	J Med Chem (2003) 46: 3853-3864 [PMID:12930147]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in Hartley guinea pig brain membrane	B	7.9	pKi	12.7	nM	Ki	J Med Chem (2008) 51: 4404-4411 [PMID:18637671]
ChEMBL	Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 1	B	8.42	pKi	3.8	nM	Ki	J Med Chem (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL	Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 1	B	8.42	pKi	3.8	nM	Ki	J Med Chem (1990) 33: 1714-1720 [PMID:2160538]
ChEMBL	The opioid receptor affinity(Ki) was evaluated by competition with [3H]DAMGO (mu) on guinea pig brain membranes	B	8.42	pKi	3.8	nM	Ki	J Med Chem (1995) 38: 402-407 [PMID:7853332]
ChEMBL	The compound was evaluated for binding affinity against opioid receptor mu in guinea pig brain membranes using [3H]- DAMGO as ligand	B	8.42	pKi	3.8	nM	Ki	J Med Chem (1992) 35: 4325-4329 [PMID:1333013]
ChEMBL	Binding affinity against mu-opioid receptor in guinea pig brain membranes	B	8.42	pKi	3.8	nM	Ki	J Med Chem (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL	Compound was evaluated for binding affinity at Opioid receptor mu 1 in guinea pig brain membranes	B	8.42	pKi	3.8	nM	Ki	J Med Chem (1991) 34: 1757-1762 [PMID:1648136]
ChEMBL	Apparent binding affinity of compound was determined by antagonism towards Opioid receptor mu 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate	F	8.49	pKi	3.2	nM	Ki	J Med Chem (2004) 47: 1400-1412 [PMID:14998329]
ChEMBL	The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by DAMGO (Opioid receptor mu 1) antagonist	F	8.49	pKi	3.2	nM	Ki	J Med Chem (2002) 45: 5378-5383 [PMID:12431065]
ChEMBL	Ability to inhibit GTP-gamma-S binding to Opioid receptor mu 1 of guinea pig caudate.	B	8.49	pKi	3.2	nM	Ki	J Med Chem (1999) 42: 1673-1679 [PMID:10229636]
ChEMBL	Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM DAMGO as the agonist ligand for mu-receptor)	F	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL	Antagonist activity against mu-opioid receptor in guinea pig ileum in the presence of morphine	F	4.95	pIC50	11200	nM	IC50	J Med Chem (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL	Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane	B	7.43	pIC50	37	nM	IC50	J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL	Antagonist activity against Opioid receptor mu 1 iin a guinea pig ileum assay	F	7.3	pA2	7.3	nM	pA2	J Med Chem (1997) 40: 3100-3108 [PMID:9301674]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL	Binding affinity against delta-opioid receptor in guinea pig brain membranes	B	10.52	pKi	0.03	nM	Ki	J Med Chem (1994) 37: 1886-1888 [PMID:8021929]
ChEMBL	Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	F	8.41	pEC50	3.9	nM	EC50	Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449]

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]