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Ligand source activities (1 row/activity)

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

(R)-Ro65-6570	3385	None	0	Human	Binding	pKi	=	-	9.60	1	8	Unclassified	Guide to Pharmacology	383.2	2	1	3	3.87	O=C1NCN(c2ccccc2)C12CCN([C@@H]1Cc3cccc4cccc1c34)CC2	https://pubmed.ncbi.nlm.nih.gov/10476866
(R)-Ro65-6570	3385	None	0	Human	Binding	Ki	=	0.25	9.60	1	8	Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor	ChEMBL	383.2	2	1	3	3.87	O=C1NCN(c2ccccc2)C12CCN([C@@H]1Cc3cccc4cccc1c34)CC2	https://dx.doi.org/10.1016/s0960-894x(99)00385-6
(R)-Ro65-6570	3385	None	0	Rat	Binding	Ki	=	0.41	9.39	-1	8	Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1	ChEMBL	383.2	2	1	3	3.87	O=C1NCN(c2ccccc2)C12CCN([C@@H]1Cc3cccc4cccc1c34)CC2	https://dx.doi.org/10.1016/s0960-894x(00)00111-6
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[(4'-bromo)benzamido]morphinan-oxalate	219960	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-1071519	4	-	PDSP KiDatabase	614.1	4	5	7	2.67	O=C(NC1CCC2(O)C3Cc4ccc(O)c5c4C2(CCN3CC2CC2)C1O5)c1ccc(Br)cc1.O=C(O)C(=O)O	-
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[(4'-iodo)benzamido]morphinan-oxalate	219961	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-2691	4	-	PDSP KiDatabase	662.1	4	5	7	2.52	O=C(NC1CCC2(O)C3Cc4ccc(O)c5c4C2(CCN3CC2CC2)C1O5)c1ccc(I)cc1.O=C(O)C(=O)O	-
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[(4'-methyl)benzamido]morphinan-oxalate	219958	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-245470	4	-	PDSP KiDatabase	550.2	4	5	7	2.22	Cc1ccc(C(=O)NC2CCC3(O)C4Cc5ccc(O)c6c5C3(CCN4CC3CC3)C2O6)cc1.O=C(O)C(=O)O	-
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[(4'-t-butyl)benzamido]morphinan-oxalate	219962	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-2691	4	-	PDSP KiDatabase	592.3	4	5	7	3.21	CC(C)(C)c1ccc(C(=O)NC2CCC3(O)C4Cc5ccc(O)c6c5C3(CCN4CC3CC3)C2O6)cc1.O=C(O)C(=O)O	-
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[(4'-trimethylfluoro)benzamido]morphinan-oxalate	219959	UNDEFINED	0	Human	Binding	pKi	=	4.20	8.38	-9	4	-	PDSP KiDatabase	604.2	4	5	7	2.93	O=C(NC1CCC2(O)C3Cc4ccc(O)c5c4C2(CCN3CC2CC2)C1O5)c1ccc(C(F)(F)F)cc1.O=C(O)C(=O)O	-
[(pF)Phe⁴]N/OFQ-(1-13)-NH₂	3073	None	0	Human	Binding	pKi	=	-	11.06	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12070757
[(pF)Phe⁴]N/OFQ-(1-13)-NH₂	3073	None	0	Human	Binding	pKi	=	-	11.06	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/15743186
[Arg¹⁴Lys¹⁵]N/OFQ	467	None	15	Human	Binding	pKi	None	-	9.50	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11097863
[Arg¹⁴Lys¹⁵]N/OFQ	467	None	15	Rat	Binding	IC50	=	0.21	9.68	-	2	Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2009.06.015
[Arg¹⁴Lys¹⁵]N/OFQ	467	None	15	Rat	Binding	IC50	=	0.21	9.68	-	2	Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2008.09.014
[F/G]N/OFQ-(1-13)-NH₂	1636	None	0	Human	Binding	pKi	None	-	9.20	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12967935
[Met]enkephalin	2495	None	37	Guinea pig	Binding	Ki	=	277.00	6.56	-186	8	Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmcl.2006.05.060
[Nphe¹]N/OFQ-(1-13)-NH₂	2875	None	0	Human	Binding	pKi	None	-	8.40	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12010780
Ac-RYYRIK-NH₂	268	None	20	Human	Binding	pKi	=	-	8.96	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9353393
Ac-RYYRIK-NH₂	268	None	20	Human	Binding	pKi	=	-	8.96	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12967935
Ac-RYYRIK-NH₂	268	None	20	Human	Binding	IC50	=	1.04	8.98	1	2	Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2014.09.018
Ac-RYYRIK-NH₂	268	None	20	Human	Binding	IC50	=	0.79	9.10	1	2	Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2007.11.043

Showing 1 to 20 of 2,070 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

(R)-Ro65-6570	3385	None	0	Human	Functional	EC50	=	39.81	7.40	-	8	Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor	ChEMBL	383.2	2	1	3	3.87	O=C1NCN(c2ccccc2)C12CCN([C@@H]1Cc3cccc4cccc1c34)CC2	https://dx.doi.org/10.1016/s0960-894x(99)00385-6
(R)-Ro65-6570	3385	None	0	Human	Functional	pEC50	=	-	7.40	-	8	Stimulation of GTP-γ³⁵S binding	Guide to Pharmacology	383.2	2	1	3	3.87	O=C1NCN(c2ccccc2)C12CCN([C@@H]1Cc3cccc4cccc1c34)CC2	https://pubmed.ncbi.nlm.nih.gov/10476866
[(pF)Phe⁴]N/OFQ-(1-13)-NH₂	3073	None	0	Human	Functional	pEC50	=	-	10.12	-	1	Stimulation of GTP-γ³⁵S binding	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/15743186
[Arg¹⁴Lys¹⁵]N/OFQ	467	None	15	Rat	Functional	EC50	=	1.10	8.96	-	2	Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2009.06.015
[Arg¹⁴Lys¹⁵]N/OFQ	467	None	15	Rat	Functional	EC50	=	1.10	8.96	-	2	Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2008.09.014
Ac-RYYRIK-NH₂	268	None	20	Human	Functional	pEC50	=	-	5.10	-	2	Stimulation of GTP-γ³⁵S binding	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9353393
Ac-RYYRIK-NH₂	268	None	20	Human	Functional	EC50	=	12.90	7.89	-	2	Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmc.2007.11.043
Ac-RYYRWK-NH₂	269	None	0	Human	Functional	pEC50	=	-	8.68	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9353393
BUPRENORPHINE	189274	None	0	Human	Functional	EC50	=	116.00	6.94	-954	8	Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	467.3	4	2	5	4.41	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	https://dx.doi.org/10.1021/jm2003238
BUPRENORPHINE	189274	None	0	Human	Functional	EC50	=	1480.00	5.83	-954	8	Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	467.3	4	2	5	4.41	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	https://dx.doi.org/10.1021/acs.jmedchem.5b00130
cebranopadol	877	None	42	Human	Functional	pEC50	=	-	7.89	-10	7	Stimulation of GTP-γ³⁵S binding	Guide to Pharmacology	378.2	2	1	2	5.11	CN(C)C1(c2ccccc2)CCC2(CC1)OCCc1c2[nH]c2ccc(F)cc12	https://pubmed.ncbi.nlm.nih.gov/24713140
cebranopadol	877	None	42	Human	Functional	EC50	=	13.00	7.89	-10	7	Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378.2	2	1	2	5.11	CN(C)C1(c2ccccc2)CCC2(CC1)OCCc1c2[nH]c2ccc(F)cc12	https://dx.doi.org/10.1021/ml500117c
CHEMBL101454	4410	None	15	Human	Functional	EC50	=	19.90	7.70	4	3	Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes	ChEMBL	326.2	2	0	2	4.15	O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1	https://dx.doi.org/10.1021/jm034249d
CHEMBL101454	4410	None	15	Human	Functional	EC50	=	20.80	7.68	4	3	Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	326.2	2	0	2	4.15	O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1	https://dx.doi.org/10.1016/j.bmcl.2013.03.101
CHEMBL101676	4451	None	0	Human	Functional	EC50	=	92.50	7.03	-	3	Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes	ChEMBL	346.2	2	0	2	3.60	O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1	https://dx.doi.org/10.1021/jm034249d
CHEMBL102900	4628	None	4	Human	Functional	EC50	=	28.70	7.54	-1	3	Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes	ChEMBL	338.2	2	0	2	4.01	O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1	https://dx.doi.org/10.1021/jm034249d
CHEMBL102900	4628	None	4	Human	Functional	EC50	=	28.70	7.54	-1	3	Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	338.2	2	0	2	4.01	O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1	https://dx.doi.org/10.1016/j.bmcl.2013.03.101
CHEMBL1076208	5489	None	0	Human	Functional	IC50	=	448.00	6.35	-	2	Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs	ChEMBL	413.3	4	1	4	3.90	CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21	https://dx.doi.org/10.1016/j.bmcl.2009.09.028
CHEMBL1076242	5496	None	0	Human	Functional	IC50	=	21.00	7.68	-	2	Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs	ChEMBL	448.3	5	1	4	2.98	CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O	https://dx.doi.org/10.1016/j.bmcl.2009.09.028
CHEMBL1079400	5870	None	0	Human	Functional	IC50	=	5.20	8.28	-	2	Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs	ChEMBL	476.3	4	1	4	3.66	CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O	https://dx.doi.org/10.1016/j.bmcl.2009.09.028

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Ligand source activities (1 row/activity)